GNE-955

发表于2024年10月31日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GNE-955

GNE-955 是有效的，可口服的泛 Pim 激酶抑制剂，对 Pim1，Pim2，Pim3 的 K_i 值分别为 0.018，0.11，0.08 nM。

GNE-955 Chemical Structure

CAS No. : 1527523-39-2

规格		是否有货
100 mg		询价
250 mg		询价
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生物活性

GNE-955 is a potent and orally active pan Pim kinase inhibitor with K_is of 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively.

IC₅₀ & Target^[1]

PIM1

0.018 nM (Ki)

PIM2

0.11 nM (Ki)

PIM3

0.08 nM (Ki)

体外研究
(In Vitro)

GNE-955 inhibits proliferation of MM.1S cells, with an IC₅₀ value of 0.5 μM after 72 hours treatment^[1].
GNE-955 (0.156-5 μM) inhibits the phosphorylation of BAD (s112), S6 (s235/236), S6 (s240/244) and 4EBP (s65), shows no effect on total BAD, S6 or 4EBP protein levels.^[1]

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

416.48

Formula

C₂₂H₂₄N₈O

CAS 号

1527523-39-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Wang X, et al. Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability. J Med Chem. 2017 May 25;60(10):4458-4473.

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GNE-6640

发表于2024年10月27日由上海金畔生物科技有限公司

GNE-6640 纯度: 99.81%

GNE-6640 是泛素特异性肽酶 7 (USP7) 选择性的、非共价结合的抑制剂，其对USP7 全长，USP7 催化结构域，USP43 全长以及 Ub-MDM2 的 IC₅₀ 值分别为 0.75 μM，0.43 μM，20.3 μM 和 0.23 μM。

GNE-6640 Chemical Structure

CAS No. : 2009273-67-8

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2310	In-stock
5 mg	￥2100	In-stock
10 mg	￥3500	In-stock
25 mg	￥7400	In-stock
50 mg	￥12000	In-stock
100 mg		询价

* Please select Quantity before adding items.

GNE-6640 相关产品

•相关化合物库:

Covalent Screening Library Plus
Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Covalent Screening Library
Ubiquitination Compound Library

生物活性

GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7), with IC₅₀ values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively.

IC₅₀ & Target

IC50: 0.75 μM(full length USP7), 0.43 μM(USP7 catalytic domain), 20.3 μM(full length USP43), 0.23 μM(Ub-MDM2)^[1].

体外研究
(In Vitro)

GNE-6640 promotes endogenous MDM2 ubiquitination with Lys48 (K48)-linked polyubiquitin chains, which directs proteasomal degradation13. GNE-6640 targets cellular USP7, MDM2, and p53 signalling pathways. GNE-6640 decreases viability of 108 cell lines with IC₅₀ ≤ 10 μM. Combining GNE-6640 with doxorubicin or cisplatin (DNA-damaging agents), which could activate the p53 response and enhance USP7 inhibitor efficacy. GNE-6640 could induce tumor cell death. GNE-6640 enhances cytotoxicity with chemotherapeutic agents and targeted compounds, including PIM kinase inhibitors^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

330.38

Formula

C₂₀H₁₈N₄O

CAS 号

2009273-67-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 5 mg/mL (15.13 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0268 mL	15.1341 mL	30.2682 mL
5 mM	0.6054 mL	3.0268 mL	6.0536 mL
10 mM	0.3027 mL	1.5134 mL	3.0268 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

参考文献

[1]. Kategaya L, et al. USP7 small-molecule inhibitors interfere with ubiquitin binding. Nature. 2017 Oct 26;550(7677):534-538.

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GNE 2861

发表于2024年10月26日由上海金畔生物科技有限公司

GNE 2861 纯度: 99.47%

GNE 2861 是 PAK 的抑制剂，对 group II 具有选择性。GNE 2861 抑制 PAK4，PAK5 和 PAK6 的 IC₅₀ 值分别为7.5，36和126 nM。

GNE 2861 Chemical Structure

CAS No. : 1394121-05-1

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1520	In-stock
1 mg	￥950	In-stock
5 mg	￥1700	In-stock
10 mg	￥2800	In-stock
25 mg	￥5600	In-stock
50 mg	￥9400	In-stock
100 mg	￥16800	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GNE 2861 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Kinase Inhibitor Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Cytoskeleton Compound Library

生物活性

GNE 2861 is a PAK inhibitor that displays group II selectivity. GNE 2861 inhibits PAK4, PAK5 and PAK6 with IC₅₀s of 7.5, 36, 126 nM, respectively.

IC₅₀ & Target

IC50: 7.5 nM (PAK4), 36 nM (PAK5), 126 nM (PAK6)^[1]

体外研究
(In Vitro)

GNE 2861 is compound 4 from the reference^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

406.48

Formula

C₂₂H₂₆N₆O₂

CAS 号

1394121-05-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (246.01 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4601 mL	12.3007 mL	24.6015 mL
5 mM	0.4920 mL	2.4601 mL	4.9203 mL
10 mM	0.2460 mL	1.2301 mL	2.4601 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (5.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.12 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2.08 mg/mL (5.12 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (5.12 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Karpov AS, et al. Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. ACS Med Chem Lett. 2015 May 22;6(7):776-81.

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GNE-140 racemate

发表于2024年10月25日由上海金畔生物科技有限公司

GNE-140 racemate 纯度: 99.66%

GNE-140 racemate 是一种 (R)-GNE-140 和 (S)-GNE-140 的外消旋混合物。GNE-140 racemate 也是一种有效的乳酸脱氢酶 A (LDHA) 抑制剂。

GNE-140 racemate Chemical Structure

CAS No. : 1802977-61-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3843	In-stock
1 mg	￥1400	In-stock
5 mg	￥3500	In-stock
10 mg	￥5000	In-stock
50 mg	￥15000	In-stock
100 mg	￥21000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GNE-140 racemate 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Glycolysis Compound Library
Anti-Cancer Metabolism Compound Library
Glucose Metabolism Compound Library
Targeted Diversity Library

生物活性

GNE-140 racemate is a racemate mixture of (R)-GNE-140 and (S)-GNE-140. GNE-140 racemate is a potent lactate dehydrogenase A (LDHA) inhibitor^[1]^[2].

IC₅₀ & Target

Lactate dehydrogenase A (LDHA)^[1]

体外研究
(In Vitro)

Increased glucose consumption distinguishes cancer cells from normal cells and is known as the “Warburg effect” because of increased glycolysis. Lactate dehydrogenase A (LDHA) is a key glycolytic enzyme, a hallmark of aggressive cancers, and believed to be the major enzyme responsible for pyruvate-to-lactate conversion^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

499.04

Formula

C₂₅H₂₃ClN₂O₃S₂

CAS 号

1802977-61-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 20 mg/mL (40.08 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0038 mL	10.0192 mL	20.0385 mL
5 mM	0.4008 mL	2.0038 mL	4.0077 mL
10 mM	0.2004 mL	1.0019 mL	2.0038 mL

参考文献

[1]. Ždralević M, et al. Double genetic disruption of lactate dehydrogenases A and B is required to ablate the “Warburg effect” restricting tumor growth to oxidative metabolism. J Biol Chem. 2018 Oct 12;293(41):15947-15961.

[2]. Purkey HE, et al. Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice. ACS Med Chem Lett. 2016 Aug 26;7(10):896-901.

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(S)-GNE-140

发表于2024年10月24日由上海金畔生物科技有限公司

(S)-GNE-140 纯度: 99.04%

(S)-GNE-140 是活性较小的 GNE-140 的对映体，能够抑制乳酸脱氢酶 A (LDHA)。

(S)-GNE-140 Chemical Structure

CAS No. : 2003234-64-6

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥6862	In-stock
1 mg	￥1980	In-stock
5 mg	￥6250	In-stock
10 mg	￥8880	In-stock
50 mg	￥26700	In-stock
100 mg	￥42090	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

(S)-GNE-140 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Glycolysis Compound Library
Anti-Cancer Metabolism Compound Library
Glucose Metabolism Compound Library
Targeted Diversity Library

生物活性

(S)-GNE-140 is the less active enantiomer of GNE-140 which can inhibit Lactate dehydrogenase A (LDHA).

IC₅₀ & Target

LDHA^[1]

分子量

499.04

Formula

C₂₅H₂₃ClN₂O₃S₂

CAS 号

2003234-64-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 14 mg/mL (28.05 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0038 mL	10.0192 mL	20.0385 mL
5 mM	0.4008 mL	2.0038 mL	4.0077 mL
10 mM	0.2004 mL	1.0019 mL	2.0038 mL

参考文献

[1]. Purkey HE, et al. Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice. ACS Med Chem Lett. 2016 Aug 26;7(10):896-901.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

GNE-617

发表于2024年10月23日由上海金畔生物科技有限公司

GNE-617 纯度: 99.85%

GNE-617是新型特异的Nampt抑制剂，在A549细胞中IC50为18.9nM。

GNE-617 Chemical Structure

CAS No. : 1362154-70-8

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥920	In-stock
2 mg	￥550	In-stock
5 mg	￥900	In-stock
10 mg	￥1500	In-stock
50 mg	￥4500	In-stock
100 mg	￥7500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GNE-617 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Anti-Lung Cancer Compound Library

生物活性

GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC₅₀ of 5 nM and exhibits efficacy in xenograft models of cancer.

IC₅₀ & Target

IC50: 5 nM (NAMPT)^[1]

体外研究
(In Vitro)

The activity ofGNE-617 hydrochloride is evaluated on a panel 53 non-small cell lung cancer (NSCLC) cell lines in the presence or absence of 10 μM nicotinic acid. GNE-617 inhibits NAMPT IC50 of 18.9 nM in A549 cell.The majority of cell lines exhibit a steep dose response to GNE-617 when evaluated by decrease in ATP or total nucleic acid, and the cytotoxicity is completely rescued by simultaneous addition of nicotinic acid. The majority of the cell lines tested have IC₅₀ values below 100 nM, with approximately half with IC₅₀ values less than 10 nM. Eighteen cell lines are not rescued with nicotinic acid, and these non-rescuable cell lines tended to have lower IC₅₀ values (P=0.008, Fisher exact test, IC₅₀<10 nm vs. ≥10 nm)^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

In rats, GNE-617 hydrochloride (administered QD) and GNE-875 (administered BID) are associated with more severe retinal toxicity at similar exposures and dosing duration compared with GMX-1778 (administered BID). The mouse efficacy studies using GNE-617, GNE-618, and GMX-1778 are designed to assess efficacy and opportunistically used to assess retinal toxicity in mice. NAMPTi retinal toxicity is observed with GNE-617 and GMX-1778; however, the different study durations between GNE-617 and GMX-1778 do not allow for direct comparison of retinal toxicity^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

427.42

Formula

C₂₁H₁₅F₂N₃O₃S

CAS 号

1362154-70-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 16.67 mg/mL (39.00 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3396 mL	11.6981 mL	23.3962 mL
5 mM	0.4679 mL	2.3396 mL	4.6792 mL
10 mM	0.2340 mL	1.1698 mL	2.3396 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 1.67 mg/mL (3.91 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (3.91 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 1.67 mg/mL (3.91 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (3.91 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Shames DS, et al. Loss of NAPRT1 Expression by Tumor-specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors. Clin Cancer Res. 2013 Dec 15;19(24):6912-23.

[2]. Zabka TS, et al. Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase. Toxicol Sci. 2015 Mar;144(1):163-72.

Kinase Assay ^[1]	For RNA interference (RNAi), A549 cells are plated at 1,500 cells per well in 96-well plates, allowed to adhere for 24 hours, and transfected with 25 nM siRNA oligonucleotide using Dharmafect 4. Transfected cells are treated with the indicated concentrations of GNE-617 (0.1, 1 , 10 , 100 , and 1000 nM) for 72 hours and viability is evaluated with CellTiter-Glo. Lysates for detection of NAPRT1 protein are collected 72 hours after transfection of 1 million A549 cells in 10 cm dishes. For NAPRT1 re-expression, RERF-LC-MS cells are transfected with pCMV6-AC.NAPRT1 and empty vector pCMV6-AC using Amaxa Nucleofector technology and selected with Geneticin^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cells are grown in RPMI-1640 medium supplemented with 10% FBS and 2 mM glutamine and passaged not more than 20 times after thawing. To determine the IC₅₀ values and nicotinic acid rescue status, cells are treated with nine point dose titrations of GNE-617 with or without 10 μM nicotinic acid. At 96 hours post-drug addition, the GNE-617-treated cells are evaluated using CyQUANT Direct Cell Proliferation Assay followed by CellTiter-Glo Luminescent Cell Viability Assay quantified with a Wallac EnVision 2104 Multilabel Reader. IC₅₀ values are calculated using XLfit 5.1. To examine the protein level, cells are lysed in ice-cold radioimmunoprecipitation assay buffer, run on SDS-PAGE (4%-12% Bis-Tris), and evaluated by Western blotting using antibodies directed against NAPRT1 and β-actin^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Rats^[2] Male naïve Sprague Dawley rats are administered once daily (QD) via oral gavage either (1) GNE-617 at 30 mg/kg for 2 consecutive days in combination with NA at 75 mg/kg twice daily (BID; 6 h apart); (2) GNE-618 at 30 mg/kg for 1 day; or (3) GMX-1778 at 30 mg/kg for 1 day. Dose selection for each compound is based on tolerability and toxicity findings from the safety studies and for nicotinic acid (NA) on the highest concentration of NA that could be administered to rats in a solution form. Formulating NA at higher concentration resulted in a suspension, and NA is determined to be unstable in a suspension form. GNE-617, GNE-618, and GMX-1778 are formulated as a solution in the vehicle of 60% polyethylene glycol (PEG 400)/10% ethanol/30% 5% dextrose in water (D5W) (vol/vol/vol), and NA is formulated as a solution in water. At 1 h and 6.5 h post-dose (on Day 2 for GNE-617), rats (3-4 rats per time point) are euthanized, and the blood, retina, and brain are collected. Blood samples are collected into K₂EDTA Microtainer tubes. The tubes are chilled on wet ice until centrifugation within 30 min of collection. Plasma is collected and transferred to 1.2 mL cluster tubes. Tissues are rinsed with phosphate-buffered saline and blotted dry using gauze. All samples are stored at more than −80°C until compound analysis. Results are expressed as an absolute concentration in retina, brain, or plasma and as a ratio of retina:plasma concentration. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Shames DS, et al. Loss of NAPRT1 Expression by Tumor-specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors. Clin Cancer Res. 2013 Dec 15;19(24):6912-23. [2]. Zabka TS, et al. Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase. Toxicol Sci. 2015 Mar;144(1):163-72.

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GNE-987

发表于2024年10月10日由上海金畔生物科技有限公司

GNE-987 纯度: 98.90%

GNE-987 是一种由von Hippel-Lindau配体和BRD4配体相连的PROTAC。GNE-987 显示皮摩尔细胞 BRD4 降解活性 (在 EOL-1 AML 细胞系中，DC₅₀=0.03 nM)。GNE-987 与 BRD4 的 BD1 和 BD2 结合，具有低纳米摩尔亲和力 (IC₅₀ 分别为 4.7 和 4.4 nM)。它包含一个有效的 BET 结合剂/抑制剂、一个 VHL 结合片段和一个十个亚甲基间隔基部分。GNE-987 用于 PROTAC-Antibody 偶联物 (PAC)中。

GNE-987 Chemical Structure

CAS No. : 2417371-71-0

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1 mg	￥5950	In-stock
5 mg	￥13500	In-stock
10 mg	￥21500	In-stock
50 mg		询价
100 mg		询价

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GNE-987 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC₅₀=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC₅₀=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC)^[1].

IC₅₀ & Target^[1]

BRD4 (BD1)

4.7 nM (IC₅₀)

BRD4 (BD2)

4.4 nM (IC₅₀)

VHL

体外研究
(In Vitro)

GNE-987 inhibits EOL-1 and HL-60 cell viability with IC₅₀s of 0.02 and 0.03 nM, respectively, and inhibits MYC expression with an IC₅₀ of 0.03 nM^[1].
GNE-987 (0.1-10 nM; 5 hours) degrades the BRD2 and BRD3 BET family proteins^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	EOL-1 cells
Concentration:	0.1, 1, 10 nM
Incubation Time:	5 hours
Result:	Degraded the BRD2 and BRD3 BET family proteins.

分子量

1096.31

Formula

C₅₆H₆₇F₂N₉O₈S₂

CAS 号

2417371-71-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

In Vitro:

DMSO : 150 mg/mL (136.82 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.9122 mL	4.5608 mL	9.1215 mL
5 mM	0.1824 mL	0.9122 mL	1.8243 mL
10 mM	0.0912 mL	0.4561 mL	0.9122 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 7.5 mg/mL (6.84 mM); Clear solution

此方案可获得 ≥ 7.5 mg/mL (6.84 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 75.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Pillow TH, et al. Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity. ChemMedChem. 2019 Oct 31.

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(R)-GNE-140

发表于2024年10月7日由上海金畔生物科技有限公司

(R)-GNE-140 纯度: 99.20%

(R)-GNE-140 是一种有效的 LDHA 抑制剂，对 LDHA 和 LDHB 的 IC₅₀ 值分别为 3 nM 和 5 nM；(R)-GNE-140 的活性是 S 型异构体的 18 倍。

(R)-GNE-140 Chemical Structure

CAS No. : 2003234-63-5

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥2200	In-stock
5 mg	￥2000	In-stock
10 mg	￥3380	In-stock
50 mg	￥9950	In-stock
100 mg	￥14000	In-stock
200 mg		询价
500 mg		询价

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(R)-GNE-140 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Glycolysis Compound Library
Anti-Cancer Metabolism Compound Library
Glucose Metabolism Compound Library
Targeted Diversity Library

生物活性

(R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC₅₀s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer.

IC₅₀ & Target

IC50: 3 nM (LDHA), 5 nM (LDHB)^[1]

体外研究
(In Vitro)

(R)-GNE-140 inhibits proliferation in 37 of 347 cancer cell lines tested at a potency cut off of 5 μM. (R)-GNE-140 shows inhibitory effect on two chondrosarcoma (bone) cancer cell lines that harbor IDH1 mutations, with the IC₅₀ of 0.8 μM^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

(R)-GNE-140 (5 mg/kg) has high bioavailability in mice. At higher oral doses, ranging from 50 to 200 mg/kg, (R)-GNE-140 displays greater exposure.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

499.04

Formula

C₂₅H₂₃ClN₂O₃S₂

CAS 号

2003234-63-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 50 mg/mL (100.19 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0038 mL	10.0192 mL	20.0385 mL
5 mM	0.4008 mL	2.0038 mL	4.0077 mL
10 mM	0.2004 mL	1.0019 mL	2.0038 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (5.01 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.01 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (5.01 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.01 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.01 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.01 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
4.

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline

Solubility: 2.5 mg/mL (5.01 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Purkey HE, et al. Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice. ACS Med Chem Lett. 2016 Aug 26;7(10):896-901.

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GNE-274

发表于2024年10月2日由上海金畔生物科技有限公司

GNE-274

GNE-274 是 ER 降解剂 GDC-0927 的结构类似物，是一种非降解剂。GNE-274 在乳腺癌细胞系中不诱导 ER 的转换，作为 ER 的部分激动剂 (partial ER agonist) 发挥作用。GNE-274 增加了ER-DNA 结合位点的的染色质可进入性，而 GDC-0927 则没有。GNE-274 是一种有效的 ER 配体结合域 (LBD) 抑制剂。GNE-274 可用于癌症研究。

GNE-274 Chemical Structure

CAS No. : 2369048-69-9

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100 mg		询价
250 mg		询价
500 mg		询价

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生物活性

GNE-274 is a non-degrader that is structurally related to GDC-0927 (ER degrader). GNE-274 does not induce ER turnover and functions as a partial ER agonist in breast cancer cell lines. GNE-274 increase chromatin accessibility at ER-DNA binding sites, while GDC-0927 do not. GNE-274 is a potent inhibitor of ER-ligand binding domain (LBD). GNE-274 can be used for cancer research^[1]^[2].

体外研究
(In Vitro)

GNE-274 (0.1 nM-1000 nM; 4 hours) fails to trigger increased ER turnover in MCF7, MD-134, HCC1500 and CAMA cells^[1].
GNE-274 (1-1000 nM; 7-10 days) potently inhibits cellular proliferation, exhibiting greater potency than fulvestrant, 4-OHT, AZD9496, and GDC-0810 in E2-stimulated ER⁺ breast cancer cell lines^[1].
In transposaseaccessible chromatin sequencing (ATAC-seq) assay, GNE-274 increase chromatin accessibility at ER-DNA binding sites, it significantly alters chromatin accessibility at 594 sites. But GDC-0927 has considerably less impact on chromatin accessibility^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	MCF7, MB-134, HCC1500, EFM-19, CAMA-1, T-47D cells
Concentration:	1 nM; 10 nM; 100 nM; 1000 nM
Incubation Time:	7-10 days
Result:	Exhibited IC₅₀ values approximately ranging from 5nM to 20 nM in different cells.

分子量

457.56

Formula

C₂₉H₃₁NO₄

CAS 号

2369048-69-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Jane Guan, et al. Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility. Cell. 2019 Aug 8;178(4):949-963.e18.

[2]. Jane Guan, et al. Abstract NG05: Not all “SERDs” are equal: Context-independent ER degradation and full ER antagonism define the next generation of ER therapeutics. Cancer research.

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GNE 220

发表于2024年9月16日由上海金畔生物科技有限公司

GNE 220

GNE-220 是一种有效的选择性 MAP4K4 抑制剂，IC₅₀ 为 7 nM。

GNE 220 Chemical Structure

CAS No. : 1199590-75-4

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GNE 220 的其他形式现货产品:

GNE 220 hydrochloride

生物活性

GNE-220 is a potent and selective inhibitor of MAP4K4 with an IC₅₀ of 7 nM.

IC₅₀ & Target

MAP4K4

7 nM (IC₅₀)

MAP4K5

9 nM (IC₅₀)

MAP4K6

1.1 μM (IC₅₀)

体外研究
(In Vitro)

GNE-220 also inhibits a few other kinases with IC₅₀s of 9 nM, 476 nM and 1.1 μM for MINK (MAP4K6), DMPK and KHS1 (MAP4K5), respectively. GNE-220 alters human umbilical vein endothelial cells (HUVEC) sprout morphology. GNE-220 also reduces pERM⁺ retraction fibres in a dose-dependent manner. GNE-220 also dose-dependently increased the number of active-INTβ1⁺ long focal adhesions (FAs)^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

438.53

Formula

C₂₅H₂₆N₈

CAS 号

1199590-75-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Vitorino P, et al. MAP4K4 regulates integrin-FERM binding to control endothelial cell motility. Nature. 2015 Mar 26;519(7544):425-30.

Kinase Assay ^[1]	His-tagged MAP4K4 kinase domain (A2-E328) is expressed and purified from SF9 insect cells. 3 μg of purified kinase containing a T181E activating mutation is incubated with 100 μM moesin peptide LGRDKYKTLRQIRQ or purified Myc-Flag-moesin in 50 mM HEPES pH 7.2/10 mM MgCl₂/1 mM EGTA/0.01% Triton X-100 for 45 min at room temperature in the presence or absence of 3 μM ATP. Remaining ATP levels are assayed using KinaseGlo^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	HUVECs are cultured in complete EGM-2 (CC-3156 and CC-4176). HUVEC are assayed 3 days after siRNA transfection. CHO cells (ATCC, CCL-61) are cultured in DMEM supplemented with 10% FBS, 1 mM Glutamate, and Penicillin/Streptomycin and transfected using Lipofectamine LTX. HUVEC sprouting assays are performed. For siRNA treatment, HUVECs are transfected 1 day before coating to beads. For chemical inhibitor (e.g., GNE-220, 0.1, 1, 10, 100, 1000 and 10000 nM) treatment, is added to media after fibrin is clotted. For immunofluorescence staining, beads are seeded in thin 100 μL fibrin clots. For scratch wound healing assay, HUVEC are transfected 2 days before re-seeding into a glass-bottom 96-wells plate^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Vitorino P, et al. MAP4K4 regulates integrin-FERM binding to control endothelial cell motility. Nature. 2015 Mar 26;519(7544):425-30.

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GNE-272

发表于2024年9月15日由上海金畔生物科技有限公司

GNE-272 纯度: 99.74%

GNE-272 是有效和选择性的 CBP/EP300 抑制剂，对 CBP，EP300 和 BRD4 的 IC₅₀ 值分别为0.02，0.03 和 13 μM。GNE-272 也是 CBP/EP300 选择性的体内探针。

GNE-272 Chemical Structure

CAS No. : 1936428-93-1

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1774	In-stock
2 mg	￥1100	In-stock
5 mg	￥1900	In-stock
10 mg	￥3000	In-stock
50 mg	￥12000	In-stock
100 mg	￥19000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GNE-272 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Chemical Probe Library
Anti-Blood Cancer Compound Library

生物活性

GNE-272 is a potent and selective CBP/EP300 inhibitor with IC₅₀ values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300^[1].

IC₅₀ & Target

IC50: 0.02 μM (CBP), 0.03 μM (EP300), 13 μM (BRD4)^[1]

体外研究
(In Vitro)

GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. When tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel, GNE-272 does not inhibit any target at >30%. In addition, GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). The compound has good potency in the BRET cellular assay. In an orthogonal measure of the target engagement, GNE-272 is shown to inhibit the expression of MYC10 (MV4−11 cell line) with an EC₅₀ of 0.91 μM and good correlation between the BRET and MYC cellular assays is observed^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GNE-272 demonstrates low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound C_max of 26 μM. GNE-272 shows a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

424.47

Formula

C₂₂H₂₅FN₆O₂

CAS 号

1936428-93-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (235.59 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3559 mL	11.7794 mL	23.5588 mL
5 mM	0.4712 mL	2.3559 mL	4.7118 mL
10 mM	0.2356 mL	1.1779 mL	2.3559 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.89 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.89 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.89 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Crawford TD, et al. Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J Med Chem. 2016 Dec 8;59(23):10549-10563.

Cell Assay ^[1]	Human cancer cell lines (MOLM-16, HL-60, LP-1, KMS-34, Pfeiffer, DOHH-2) are treated for 4 h with 5 μM GNE-272 or DMSO control. After 6 days, cell viability is measured by CellTiter-Glo^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: Mice are given 0 (vehicle, 0.5% methylcellulose; 0.2% Tween-80), 12.5, 25, and 50 mg/kg of GNE-272 by gavage, twice daily (BID) for 21 days in a volume of 100 μL. Tumor volumes are measured in two dimensions (length and width) using Ultra CalIV calipers and analyzed using Excel, version 11.2^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Crawford TD, et al. Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J Med Chem. 2016 Dec 8;59(23):10549-10563.

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GNE 220 hydrochloride

发表于2024年9月1日由上海金畔生物科技有限公司

GNE 220 hydrochloride 纯度: 98.33%

GNE 220 (hydrochloride) 是一种有效的选择性 MAP4K4 抑制剂，其 IC₅₀ 值为 7 nM。

GNE 220 hydrochloride Chemical Structure

CAS No. : 2448286-21-1

规格	价格	是否有货
5 mg	￥6500	In-stock
10 mg	￥12000	In-stock
25 mg	￥26000	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

GNE 220 hydrochloride 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
Kinase Inhibitor Library
MAPK Compound Library
Anti-Cancer Compound Library
Oxygen Sensing Compound Library
Targeted Diversity Library

生物活性

GNE 220 (hydrochloride) is a potent and selective inhibitor of MAP4K4, with an IC₅₀ of 7 nM.

IC₅₀ & Target

MAP4K4

7 nM (IC₅₀)

MAP4K5

9 nM (IC₅₀)

MAP4K6

1.1 μM (IC₅₀)

DMPK

476 nM (IC₅₀)

体外研究
(In Vitro)

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

474.99

Formula

C₂₅H₂₇ClN₈

CAS 号

2448286-21-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 5.4 mg/mL (11.37 mM; Need ultrasonic)

H₂O : 5 mg/mL (10.53 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1053 mL	10.5265 mL	21.0531 mL
5 mM	0.4211 mL	2.1053 mL	4.2106 mL
10 mM	0.2105 mL	1.0527 mL	2.1053 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 0.54 mg/mL (1.14 mM); Clear solution

此方案可获得 ≥ 0.54 mg/mL (1.14 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 5.4 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 0.54 mg/mL (1.14 mM); Clear solution

此方案可获得 ≥ 0.54 mg/mL (1.14 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 5.4 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 0.54 mg/mL (1.14 mM); Clear solution

此方案可获得 ≥ 0.54 mg/mL (1.14 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 5.4 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Vitorino P, et al. MAP4K4 regulates integrin-FERM binding to control endothelial cell motility. Nature. 2015 Mar 26;519(7544):425-30.

Cell Assay
^[1]

HUVECs are cultured in complete EGM-2 (CC-3156 and CC-4176). HUVEC are assayed 3 days after siRNA transfection. CHO cells are cultured in DMEM supplemented with 10% FBS, 1 mM Glutamate, and Penicillin/Streptomycin and transfected using Lipofectamine LTX. HUVEC sprouting assays are performed. For siRNA treatment, HUVECs are transfected 1 day before coating to beads. For chemical inhibitor (e.g., GNE-220, 0.1, 1, 10, 100, 1000 and 10000 nM) treatment, is added to media after fibrin is clotted. For immunofluorescence staining, beads are seeded in thin 100 μL fibrin clots. For scratch wound healing assay, HUVEC are transfected 2 days before re-seeding into a glass-bottom 96-wells plate^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Vitorino P, et al. MAP4K4 regulates integrin-FERM binding to control endothelial cell motility. Nature. 2015 Mar 26;519(7544):425-30.

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GNE-495

发表于2024年7月24日由上海金畔生物科技有限公司

GNE-495 纯度: 99.68%

GNE-495 是有效，选择性的 MAP4K4 抑制剂，IC₅₀ 值3.7 nM。

GNE-495 Chemical Structure

CAS No. : 1449277-10-4

规格	价格	是否有货
1 mg	￥800	In-stock
5 mg	￥1200	In-stock
10 mg	￥1800	In-stock
50 mg	￥4500	In-stock
100 mg	￥7500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GNE-495 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
Kinase Inhibitor Library
MAPK Compound Library
Anti-Cancer Compound Library
Oxygen Sensing Compound Library
Targeted Diversity Library

生物活性

GNE-495 is a potent and selective MAP4K4 inhibitor with an IC₅₀ of 3.7 nM.

IC₅₀ & Target^[1]

MAP4K4

3.7 nM (IC₅₀)

体外研究
(In Vitro)

GNE-495 is a potent and selective MAP4K4 inhibitor with efficacy in retinal angiogenesis. GNE-495 shows the best balance of MAP4K4 inhibition, permeability, microsomal stability, and cellular potency^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GNE-495 is administered intraperitoneally to neonatal mouse pups at high doses: 25 and 50 mg/kg. GNE-495 shows good in vivo profile in all species tested, with low clearances, moderate terminal half-lives, and reasonable oral exposure levels (F=37-47%)^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

405.42

Formula

C₂₂H₂₀FN₅O₂

CAS 号

1449277-10-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 2.17 mg/mL (5.35 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4666 mL	12.3329 mL	24.6658 mL
5 mM	0.4933 mL	2.4666 mL	4.9332 mL
10 mM	—	—	—

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 0.22 mg/mL (0.54 mM); Clear solution

此方案可获得 ≥ 0.22 mg/mL (0.54 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 2.2 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 0.22 mg/mL (0.54 mM); Clear solution

此方案可获得 ≥ 0.22 mg/mL (0.54 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 2.2 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 0.22 mg/mL (0.54 mM); Clear solution

此方案可获得 ≥ 0.22 mg/mL (0.54 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 2.2 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Ndubaku CO et al. Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis. ACS Med Chem Lett. 2015 Jun 29;6(8):913-8.

Animal Administration
^[1]

Rats, Mice and Pups ^[1]
For the brain cassette study, three male Sprague-Dawley (SD) rats are dosed with intravenous (IV) bolus of six test compounds (e.g., GNE-495; 0.5 mg/kg). For the mouse PK study, female CD-1 mice are administered IV bolus doses of GNE-495 (1 mg/kg). In addition, female CD-1 mice are administered GNE-495 (5 mg/kg) via oral (PO) gavage. A dosing volume of 2 mL/kg is used for the rat brain cassette PK and 5 mL/kg is used for all other dosing. Animals are not fasted prior to dose administration, and water and food are available ad libitum. Following administration of the compound of interest, three blood samples (~60 μL) are collected at each time point from individual mice up to either 9 or 24 hours post-dose using a serial sampling approach. Immediately upon collection, the blood is mixed with K2EDTA and stored on ice or in a chilled Kryorack prior to centrifugation to obtain plasma. Within 1 hr of collection, blood samples are centrifuged at approximately 1000-2000× g for 10-15 min at 4°C, and plasma is harvested. The plasma samples are stored at -70 to -80°C until analysis. For neonate PK, 3-day old CD1 pups are injected with 25 mg/kg and 50 mg/kg GNE-495 intraperitoneally, blood samples are collected at the time points indicated, retinas are collected one hour post-dose and snap frozen in liquid nitrogen and stored at -80°C until analysis. Plasma and retinal lysate concentrations are determined by LC/MS/MS.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Ndubaku CO et al. Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis. ACS Med Chem Lett. 2015 Jun 29;6(8):913-8.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

GNE684

发表于2024年7月20日由上海金畔生物科技有限公司

GNE684

GNE684 是一种有效的受体相互作用蛋白 1 (RIP1) 抑制剂，作用于人类、小鼠与大鼠 RIP1 的 K_i^app 值分别为 21 nM、189 nM 和 691 nM。

GNE684 Chemical Structure

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean K_i^app values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively^[1].

IC₅₀ & Target

IC50: 21 nM (human RIP1), 189 nM (mouse RIP1), 691 nM (rat RIP1)^[1]

体外研究
(In Vitro)

GNE684 (20 μM; 20 hours) inhibits RIP1 kinase driven cell death effectively in several human and mouse cell lines^[1].
GNE684 (20 μM; 0-60 minutes) disrupts TBZ (2 μM BV6, 20 ng/ml TNF, 20 μM zVAD)-induced RIP1 autophosphorylation, interactions between RIP1 and RIP3, RIP3 autophosphorylation, and phosphorylation of MLKL by RIP3^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	L929 cells, Jurkat cells, MEFs
Concentration:	20 μM
Incubation Time:	20 hours
Result:	Inhibited RIP1 kinase driven cell death effectively in several human and mouse cell lines.

Western Blot Analysis^[1]

Cell Line:	HT-29 cells, J774A.1 cells
Concentration:	0 μM, 20 μM
Incubation Time:	0 minute, 15 minutes, 60 minutes
Result:	Disrupted TBZ (2 μM BV6, 20 ng/ml TNF, 20μM zVAD)-induced RIP1 autophosphorylation, interactions between RIP1 and RIP3, RIP3 autophosphorylation, and phosphorylation of MLKL by RIP3.

体内研究
(In Vivo)

GNE684 also had no impact on overall survival or tumor growth in the KPP or KPR (LSL-Kras^G12D/+; p16/p19^fl/wt; Trp53^R270H/wt; Pdx1-cre) PDAC models^[1].
GNE684 (50mg/kg; p.o. twice daily) inhibits colitis and ileitis caused by NEMO deficiency in intestinal epithelial cells (IECs)^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nemo^fl/fl Villin.creERT2 mice (NEMO IEC-KO)^[1]
Dosage:	50 mg/kg
Administration:	Oral administration; twice daily; from days 2–6 treated with tamoxifen
Result:	Almost completely protected the NEMO-deficient intestines from colitis and ileitis.

分子量

432.48

Formula

C₂₃H₂₄N₆O₃

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Patel S, et al. RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases. Cell Death Differ. 2019 May 17.

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GNE-781

发表于2024年7月16日由上海金畔生物科技有限公司

GNE-781 纯度: 98.21%

GNE-781 是一种有效的，具有口服活性的选择性 CBP 抑制剂，在 TR-FRET 实验中 IC₅₀ 为 0.94 nM。GNE-781 还抑制 BRET 和 BRD4 (1)，IC₅₀ 分别为 6.2 nM 和 5100 nM。GNE-781 在 MOLM-16 AML 异种移植模型中显示抗肿瘤活性。

GNE-781 Chemical Structure

CAS No. : 1936422-33-1

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3700	In-stock
5 mg	￥3200	In-stock
10 mg	￥5200	In-stock
50 mg	￥15200	In-stock
100 mg	￥24300	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GNE-781 相关产品

•相关化合物库:

Covalent Screening Library Plus
Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Covalent Screening Library
Reprogramming Compound Library
Orally Active Compound Library
Chemical Probe Library
Anti-Blood Cancer Compound Library

生物活性

GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC₅₀ of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC₅₀s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model^[1].

IC₅₀ & Target

IC50: 0.94 nM (CBP), 6.2 nM (BRET), 5100 nM (BRD4(1))^[1]

体外研究
(In Vitro)

GNE-781 is a highly advanced potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein, binding protein (CBP). GNE-781 reduces FOXP3 (forkhead box P3) transcript levels. Examination of a subset of bromodomains reveals that GNE-781 is exquisitely selective for CBP/P300 and is remarkably selective for CBP (5425-fold) and P300 (4250-fold). GNE-781 demonstrates an appropriate balance of cell potency, selectivity (5425-fold over BRD4(1)) ^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GNE-781 (3-30 mg/kg; p.o.; twice daily for 21 days) has tumor growth inhibition (%TGI) is 73%, 71%, and 89% at 3, 10, and 30 mg/kg, respectively in SCID beige mice with MOLM-16 AML xenografts^[1].
GNE-781 decreases Foxp3 transcript levels in a dose dependent manner. GNE-781 (3-30 mg/kg) suppresses MYC at doses as low as 3 mg/kg at 2 and 8 h, with maximal suppression at 10 and 30 mg/kg at 2 h (87% and 88% inhibition, respectively)^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

525.59

Formula

C₂₇H₃₃F₂N₇O₂

CAS 号

1936422-33-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

In Vitro:

DMSO : 100 mg/mL (190.26 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9026 mL	9.5131 mL	19.0262 mL
5 mM	0.3805 mL	1.9026 mL	3.8052 mL
10 mM	0.1903 mL	0.9513 mL	1.9026 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline

Solubility: ≥ 2.87 mg/mL (5.46 mM); Clear solution
2.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)

Solubility: 2.87 mg/mL (5.46 mM); Suspended solution; Need ultrasonic
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 1.67 mg/mL (3.18 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (3.18 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
4.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1.67 mg/mL (3.18 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (3.18 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
5.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 1.67 mg/mL (3.18 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (3.18 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Romero FA, et al. GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). J Med Chem. 2017 Nov 22;60(22):9162-9183.

Animal Administration
^[1]

Mice^[1]
Twelve female CD-1 mice are used. All animals are 6-9 weeks old at the time of study and weighed between 20 and 35 g. Animals (n=3 per dosing route) are dosed with 10 or GNE-781 at 1 mg/kg iv (in propyl ethylene glycol 400 (35% v/v) and water (65% v/v)) or 5 mg/kg po (suspended in 0.5% w/v methylcellulose, 0.2% w/v Tween 80). Food and water are available ad libitum to all animals. Serial blood samples (15 μL) are collected by tail nick at 0.033, 0.083, 0.25, 0.5, 1, 3, 8, and 24 h after the intravenous administration and 0.083, 0.25, 0.5, 1, 3, 8, and 24 h after the oral administration. All blood samples are diluted with 60 μL of water containing 1.7 mg/mL EDTA and kept at -80 °C until analysis^[1].
Rats^[1]
Twelve male Sprague-Dawley rats are used. All animals are 6-9 weeks old at the time of study and weighed between 200 and 300 g. Animals (n=3 per dosing route) are dosed with 10 or GNE-781 at 1 mg/kg iv (in propyl ethylene glycol 400 (35% v/v) and water (65% v/v)) or 5 mg/kg po (suspended in 0.5% w/v methylcellulose, 0.2% w/v Tween 80). Food and water are available ad libitum to animals in the iv groups. Animals in po groups are fasted overnight and food withheld until 4 h postdose. Approximately 250 μL of blood are collected via the catheter at 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 8, and 24 h after the intravenous or oral administration. All blood samples are collected into tubes containing 5 μL of 0.5 M K₂EDTA and processed for plasma. Samples are centrifuged (2500g for 15 min at 4°C) within 1 h of collection, and plasma samples are kept at -80 °C until analysis^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Romero FA, et al. GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). J Med Chem. 2017 Nov 22;60(22):9162-9183.

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GNE-207

发表于2024年7月12日由上海金畔生物科技有限公司

GNE-207 纯度: 98.10%

GNE-207 是一种有效、选择性、可口服的 CBP 溴结构域抑制剂，IC₅₀ 值为 1 nM，对其选择性是的 BRD4 (1) 的 2500 多倍。在 MV-4-11 细胞中，GNE-207 对 MYC 表达具有高效活性，EC₅₀ 值为 18 nM。

GNE-207 Chemical Structure

CAS No. : 2158266-58-9

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Bioactive Compound Library Plus

生物活性

GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC₅₀ of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC₅₀ of 18 nM for MYC expression in MV-4-11 cells^[1].

IC₅₀ & Target^[1]

CBP

1 nM (IC₅₀)

BRD4(1)

3.1 μM (IC₅₀)

体外研究
(In Vitro)

GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC₅₀ of 1 nM, a selectively index of >2500-fold against BRD4 (1) (IC₅₀, 3.1 μM)^[1].
GNE-207 shows excellent CBP potency, with an EC₅₀ of 18 nM for MYC expression in MV-4-11 cells^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GNE-207 (5 mg/kg) shows moderate clearance in PK, with acceptable oral bioavailability^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

510.59

Formula

C₂₉H₃₀N₆O₃

CAS 号

2158266-58-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 200 mg/mL (391.70 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9585 mL	9.7926 mL	19.5852 mL
5 mM	0.3917 mL	1.9585 mL	3.9170 mL
10 mM	0.1959 mL	0.9793 mL	1.9585 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 5 mg/mL (9.79 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.79 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 5 mg/mL (9.79 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.79 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 5 mg/mL (9.79 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.79 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Lai KW, et al. Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300. ioorg Med Chem Lett. 2018 Jan 1;28(1):15-23.

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GNE-618

发表于2024年7月7日由上海金畔生物科技有限公司

GNE-618 纯度: 98.14%

GNE-618 是一种有效的，具有口服活性的烟酰胺磷酸核糖基转移酶 (NAMPT) 抑制剂，IC₅₀ 为 6 nM。GNE-618 消耗 NAD 水平并诱导细胞死亡，具有抗肿瘤活性。

GNE-618 Chemical Structure

CAS No. : 1362151-42-5

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10 mM * 1 mL in DMSO	￥2230	In-stock
5 mg	￥2200	In-stock
10 mg	￥3300	In-stock
25 mg	￥6600	In-stock
50 mg	￥10000	In-stock
100 mg	￥15000	In-stock
250 mg	￥26000	In-stock
500 mg		询价
1 g		询价

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生物活性

GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC₅₀ of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity^[1].

IC₅₀ & Target

IC50: 6 nM (NAMPT)^[1]

体外研究
(In Vitro)

GNE-618 reduces levels of NAD with an EC₅₀ of 2.6 nM in the NSCLC cell line Calu-6^[1].
GNE-618 (10-30 nM; 72 hours) reveals an increase in the sub-2N population and a decreases in the percentage of cells in the G1 and M phases of the cell cycle in Calu-6 cells^[1].
GNE-618 also reduces cellular proliferation of Calu-6 cells as determined using two different assay formats, either measuring ATP (EC₅₀ of 13.6 ± 1.8 nM) or total protein content (SRB assay; EC₅₀ of 25.8 ± 4.2 nM)^[1]

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GNE-618 (100 mg/kg; p.o.; twice daily for 5 days) significantly inhibits tumor growth by 88% and has minimal effects on body weight in STO#81 patient-derived gastric model^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

460.43

Formula

C₂₁H₁₅F₃N₄O₃S

CAS 号

1362151-42-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 125 mg/mL (271.49 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1719 mL	10.8594 mL	21.7188 mL
5 mM	0.4344 mL	2.1719 mL	4.3438 mL
10 mM	0.2172 mL	1.0859 mL	2.1719 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (4.52 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.52 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.52 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.52 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.52 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.52 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Xiao Y, et al. Dependence of tumor cell lines and patient-derived tumors on the NAD salvage pathway rendersthem sensitive to NAMPT inhibition with GNE-618. Neoplasia. 2013 Oct;15(10):1151-60.

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(S)-GNE-987

发表于2024年7月2日由上海金畔生物科技有限公司

(S)-GNE-987

(S)-GNE-987 (compound 4)，GNE-987 (BET 降解剂) 的羟脯氨酸差向异构体，可消除与 von Hippel-Lindau 的结合，不能降解 BRD4 蛋白。(S)-GNE-987 结合 BRD4 BD1 (IC₅₀=4 nM) 和 BD2 (3.9 nM) 溴结构域，可用于设计PROTAC-Antibody 偶联物 (PAC)。

(S)-GNE-987 Chemical Structure

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生物活性

(S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to von Hippel-Lindau and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC₅₀=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC)^[1].

IC₅₀ & Target^[1]

BRD4 (BD1)

4 nM (IC₅₀)

BRD4 (BD2)

3.9 nM (IC₅₀)

VHL

分子量

1096.31

Formula

C₅₆H₆₇F₂N₉O₈S₂

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Pillow TH, et al. Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity. ChemMedChem. 2019 Oct 31.

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GNE-317

发表于2024年5月27日由上海金畔生物科技有限公司

GNE-317 纯度: 99.31%

GNE-317 是一种 PI3K/mTOR 抑制剂，能够穿过血脑屏障 (BBB)。

GNE-317 Chemical Structure

CAS No. : 1394076-92-6

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥957	In-stock
5 mg	￥870	In-stock
10 mg	￥1500	In-stock
50 mg	￥4200	In-stock
100 mg	￥5200	In-stock
200 mg		询价
500 mg		询价

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Anti-Cancer Metabolism Compound Library
Angiogenesis Related Compound Library
Glucose Metabolism Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

GNE-317 is a PI3K/mTOR inhibitor, is able to cross the blood-brain barrier (BBB).

IC₅₀ & Target^[1]

PI3K

mTOR

体外研究
(In Vitro)

GNE-317 is an oxetane derivative of GDC-0980 synthesized with the goal of reducing substrate affinity for efflux transporters. In vitro, GDC-0980 and GNE-317 demonstrate similar profiles in MTS cytotoxicity experiments using the GL261 cell line^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Seven days after i.c. inoculation with GL261-GFP-Luc cells, mice are treated once daily with the maximum tolerated dose of GDC-0980 (7.5 mg/kg), GNE-317 (30 mg/kg), or vehicle. For GL261, tumor growth is tracked through bioluminescence imaging on a weekly basis. There are no significant changes in GL261 tumor growth among the 3 groups. In assessing survival benefits in GL261, neither GDC-0980 nor GNE-317 provides survival benefit over the vehicle-treated animals. The fact that these drugs are not effective in vivo is suggested by the in vitro cytotoxicity data showing that the drugs have limited efficacy in inducing cell death in the GL261 cell line. Neither drug is effective in the GL261 tumor in spite of greater delivery and enhanced therapeutic targeting efficacy of GNE-317^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

414.48

Formula

C₁₉H₂₂N₆O₃S

CAS 号

1394076-92-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 20 mg/mL (48.25 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4127 mL	12.0633 mL	24.1266 mL
5 mM	0.4825 mL	2.4127 mL	4.8253 mL
10 mM	0.2413 mL	1.2063 mL	2.4127 mL

参考文献

[1]. Salphati L, et al. Distribution of the phosphatidylinositol 3-kinase inhibitors Pictilisib (GDC-0941) and GNE-317 in U87 and GS2 intracranial glioblastoma models-assessment by matrix-assisted laser desorption ionization imaging. Drug Metab Dispos. 2014 Jul;42(7):1110-6.

[2]. Becker CM, et al. Decreased affinity for efflux transporters increases brain penetrance and molecular targeting of a PI3K/mTOR inhibitor in a mouse model of glioblastoma. Neuro Oncol. 2015 Sep;17(9):1210-9.

Cell Assay ^[1]	GL261 is an aggressive C57BL/6J-derived glioma line. This cell line is transfected with both green fluorescent protein (GFP) and luciferase (Luc) from separate plasmids. The resultant monoclonal GL261-GFP-Luc cells are maintained in Dulbecco’s modified Eagle’s medium supplemented with 10% FBS and Penicillin/Streptomycin (100 U/mL) and cultured at 5% oxygen. Cell selection used 4 mg/mL Puromycin and 4 mg/mL G418. Cellular viability assays are set up in a 96-well format with 2000 cells plated per well in the culture conditions. Cells are incubated in the presence of drug or vehicle for 48 hours, and viability was assessed by MTS assay. Absorbance at 490 nm is used to determine viability and at 650 nm to account for background using a Synergy Mx automated plate reader. Numerical values from drug-treated wells are normalized to the values of vehicle-treated wells to yield percent survival^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] GL261-GFP-Luc cells are implanted into 7-week-old C57BL/6J mice. When tumors reach 5e7 photons/s/cm²/sr (radiance), animals are orally administered the maximum tolerated dose of GDC-0980 (7.5 mg/kg), GNE-317 (30 mg/kg) or vehicle once a day for 3 days. The maximum tolerated doses are defined as the greatest dose that could be administered to mice with <10% drop in bodyweight. Even at these different doses, both doses provide similar plasma concentrations and thus the same overall systemic exposure. At 1 or 6 hours after the third dose, mice are euthanized with carbon dioxide and perfused with 30 mL PBS. With the aid of GFP goggles, brains are dissected into tumor core, tumor rim, and normal brain tissue. Tissue samples and blood are processed, and tissue specimens from each group are analyzed for drug concentrations using LC-MS/MS. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Salphati L, et al. Distribution of the phosphatidylinositol 3-kinase inhibitors Pictilisib (GDC-0941) and GNE-317 in U87 and GS2 intracranial glioblastoma models-assessment by matrix-assisted laser desorption ionization imaging. Drug Metab Dispos. 2014 Jul;42(7):1110-6. [2]. Becker CM, et al. Decreased affinity for efflux transporters increases brain penetrance and molecular targeting of a PI3K/mTOR inhibitor in a mouse model of glioblastoma. Neuro Oncol. 2015 Sep;17(9):1210-9.

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Piperidine-GNE-049-N-Boc

发表于2024年5月27日由上海金畔生物科技有限公司

Piperidine-GNE-049-N-Boc 纯度: 98.82%

Piperidine-GNE-049-N-Boc 是一种 dCBP-1 (HY-134582) 的 PROTAC 靶蛋白的配体。dCBP-1 是一种有效且选择性的 p300/CBP 异双功能降解剂。

Piperidine-GNE-049-N-Boc Chemical Structure

CAS No. : 1936431-36-5

规格	价格	是否有货
5 mg	￥9500	In-stock
10 mg	￥16500	In-stock
50 mg		询价
100 mg		询价

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生物活性

Piperidine-GNE-049-N-Boc is a ligand for target protein for PROTAC of dCBP-1 (HY-134582). dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP^[1].

体外研究
(In Vitro)

Piperidine-GNE-049-N-Boc (S17) can be used for synthesizing dCBP-1^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

567.67

Formula

C₃₀H₃₉F₂N₇O₂

CAS 号

1936431-36-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:

1M HCl : 32.5 mg/mL (57.25 mM; ultrasonic and adjust pH to 1 with HCl)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7616 mL	8.8079 mL	17.6159 mL
5 mM	0.3523 mL	1.7616 mL	3.5232 mL
10 mM	0.1762 mL	0.8808 mL	1.7616 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

参考文献

[1]. Vannam R, et, al. Targeted degradation of the enhancer lysine acetyltransferases CBP and p300. Cell Chem Biol. 2020 Dec 31;S2451-9456(20)30513-4.

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