BRD7-IN-1 free base

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。

BRD7-IN-1 free base 

BRD7-IN-1 free base 是一种修饰的 BI7273 衍生物 (BRD7/9 抑制剂),通过与 VHL 配体连接形成 PROTAC VZ185 (VZ185 抑制 BRD7/9 的 DC50 分别是 4.5 nM、1.8 nM)。

BRD7-IN-1 free base

BRD7-IN-1 free base Chemical Structure

CAS No. : 2305379-66-0

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生物活性

BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively)[1].

IC50 & Target

BRD7, BRD9[1]

分子量

394.47

Formula

C22H26N4O3

CAS 号

2305379-66-0

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]. Zoppi V, et al. Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7. J Med Chem. 2019 Jan 24;62(2):699-726.

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ZEN-3219

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。

ZEN-3219 

ZEN-3219 是一种 BET 抑制剂,抑制 BRD4(BD1)BRD4(BD2)BRD4(BD1BD2)IC50 分别为 0.48, 0.16 和 0.47 μM。ZEN-3219 可用于形成 PROTAC 分子,从而诱导 BRD4 降解。

ZEN-3219

ZEN-3219 Chemical Structure

CAS No. : 1952264-34-4

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生物活性

ZEN-3219 is a BET inhibitor with IC50s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4[1].

IC50 & Target[1]

BRD4 (BD1)

0.48 μM (IC50)

BRD4 (BD2)

0.16 μM (IC50)

BRD4(BD1BD2)

0.47 μM (IC50)

分子量

322.36

Formula

C19H18N2O3

CAS 号

1952264-34-4

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]. Kharenko OA, et al. Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine. J Med Chem. 2018 Sep 27;61(18):8202-8211.

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ZEN-3862

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。

ZEN-3862 

ZEN-3862 是一种 BET 抑制剂,抑制 BRD4(BD1)BRD4(BD2)IC50 分别为 0.16 和 0.13 μM。ZEN-3862 可用于形成 PROTAC 分子,从而诱导 BRD4 降解。

ZEN-3862

ZEN-3862 Chemical Structure

CAS No. : 1952264-33-3

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生物活性

ZEN-3862 is a BET inhibitor with IC50s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively. ZEN-3862 can be used to form PROTACs to induce degradation of BRD4[1].

IC50 & Target[1]

BRD4 (BD1)

0.16 μM (IC50)

BRD4 (BD2)

0.13 μM (IC50)

分子量

340.35

Formula

C19H17FN2O3

CAS 号

1952264-33-3

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]. Kharenko OA, et al. Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine. J Med Chem. 2018 Sep 27;61(18):8202-8211.

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PROTAC BRD4 Degrader-9

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。

PROTAC BRD4 Degrader-9 

PROTAC BRD4 Degrader-9 (compound 8a) 是一种有效的由von Hippel-Lindau配体和BRD4配体相连的PROTAC。PROTAC BRD4 Degrader-9 可与 STEAP1 和 CLL1 抗体偶联从而降解 PC3 前列腺癌细胞中的 BRD4 蛋白,DC50 值分别为 0.86 nM 和 7.6 nM。

PROTAC BRD4 Degrader-9

PROTAC BRD4 Degrader-9 Chemical Structure

CAS No. : 2417370-42-2

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生物活性

PROTAC BRD4 Degrader-9 (compound 8a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-9 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.86 nM and 7.6 nM, respectively[1].

IC50 & Target

BRD4[1]

分子量

1312.50

Formula

C59H71F2N9O15S4

CAS 号

2417370-42-2

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]. Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607.

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A1874

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。

A1874  纯度: 99.28%

A1874 是一种以 nutlin(MDM2 配体)为基础的、BRD4-降解的 PROTAC,DC50 值为 32 nM (诱导细胞内的 BRD4 降解)。有效抑制多种癌细胞增殖。

A1874

A1874 Chemical Structure

CAS No. : 2064292-12-0

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5 mg ¥5900 In-stock
10 mg ¥8500 In-stock
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A1874 相关产品

相关化合物库:

  • Bioactive Compound Library Plus

生物活性

A1874 is a nutlin-based (MDM2 ligand) and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation[1].

IC50 & Target[1]

BRD4

 

体外研究
(In Vitro)

Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) induces a dose-dependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nmol/L and a maximum degradation (Dmax) of BRD4 of 98% of the levels in control (0.1% DMSO-treated) cells[1].
Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) increases p53 levels in the HCT116 cells and showed dose-dependent p53 stabilization[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: HCT116 cells.
Concentration: 0-10 μM.
Incubation Time: 24 hours.
Result: Induced a dosedependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nM.
Increased p53 levels and showed dose-dependent p53 stabilization.

分子量

1173.59

Formula

C58H62Cl3F2N9O7S

CAS 号

2064292-12-0

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 (127.81 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.8521 mL 4.2604 mL 8.5209 mL
5 mM 0.1704 mL 0.8521 mL 1.7042 mL
10 mM 0.0852 mL 0.4260 mL 0.8521 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:

——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: ≥ 2.5 mg/mL (2.13 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.13 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% corn oil

    Solubility: ≥ 2.5 mg/mL (2.13 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.13 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]. Hines J, et al. MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53. Cancer Res. 2019 Jan 1;79(1):251-262.

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BRD7389

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。

BRD7389 

BRD7389 是一种特异性的 RSK 家族激酶抑制剂,对 RSK1RSK2RSK3IC50 分别为 1.5 μM,2.4 μM 和 1.2 μM。BRD7389 可以诱导胰腺 α 细胞中胰岛素表达。

BRD7389

BRD7389 Chemical Structure

CAS No. : 376382-11-5

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10 mg ¥7200 询问价格 & 货期

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生物活性

BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells[1].

IC50 & Target[1]

RSK1

1.5 μM (IC50)

RSK2

2.4 μM (IC50)

RSK3

1.2 μM (IC50)

CDK5/p35

6.5 μM (IC50)

DRAK1

2.8 μM (IC50)

FLT3

3.5 μM (IC50)

PIM1

3.7 μM (IC50)

PKG1α

6.5 μM (IC50)

SGK

13.8 μM (IC50)

体外研究
(In Vitro)

BRD7389 (0.425-6.8 μM) induces insulin expression in mouse α-cells after 3 days treatment. BRD7389 induces a dose-dependent up-regulation of insulin (Ins2) mRNA, peaking at 0.85 μM; 5 days treatment with BRD7389 results in greater induction of insulin gene expression, about 50-fold at 0.85 μM[1].
BRD7389 (0.85-6.8μM) significantly up-regulates Pdx1 mRNA expression in mouse α-cell line[1].
BRD7389 also increases β-cell-specific gene expression in primary human islet cells[1].
BRD7389 (1 μM; added 30 min prior to Carbachol treatment 48 h) fully abolishes carbachols timulated cell proliferation, but has little effect on the basal level of proliferation[2].

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

RT-PCR[1]

Cell Line: Mouse α-cell line
Concentration: 0.425, 0.85, 1.7, 3.4, 6.8 μM
Incubation Time: 3 days and 5 days
Result: Up-regulated expression of Pdx1.

Cell Proliferation Assay[2]

Cell Line: SNU-407 colon cancer cell
Concentration: 1 μM
Incubation Time: Added 30 min prior to Carbachol treatment (48 h)
Result: Almost completely blocked Carbachol (1 mM)-stimulated cell proliferation.

分子量

366.41

Formula

C24H18N2O2

CAS 号

376382-11-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

参考文献
  • [1]. Fomina-Yadlin D, et al. Small-molecule inducers of insulin expression in pancreatic alpha-cells. Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15099-104.

    [2]. Park YS, et al. EGFR and PKC are involved in the activation of ERK1/2 and p90 RSK and the subsequent proliferation of SNU-407 colon cancer cells by muscarinic acetylcholine receptors. Mol Cell Biochem. 2012 Nov;370(1-2):191-8.

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MZ 1

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。

MZ 1  纯度: 99.43%

MZ 1 是由von Hippel-Lindau配体和BRD4配体相连的PROTAC。MZ 1 强效迅速地诱导 BRD4 降解,选择性高于 BRD2 和 BRD3。对 BRD4 BD1/2,BRD3 BD1/2 和 BRD2 BD1/2 的 Kd 分别为 382/120,119/115 和 307/228 nM。

MZ 1

MZ 1 Chemical Structure

CAS No. : 1797406-69-9

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1 mg ¥600 In-stock
5 mg ¥2000 In-stock
10 mg ¥3800 In-stock
50 mg ¥7150 In-stock
100 mg   询价  
200 mg   询价  

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MZ 1 相关产品

相关化合物库:

  • Bioactive Compound Library Plus

生物活性

MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. Kds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively[1].

IC50 & Target

Kd: 382/120 nM (BRD4 BD1/2), 119/115 nM (BRD3 BD1/2), 307/228 nM (BRD2 BD1/2)[1].

体外研究
(In Vitro)

MZ 1 conjugates the pan-BET inhibitor JQ1 to VH032, a potent and specific VHL ligand, via a 3-unit PEG linker[2].
MZ 1 (100 and 250 nM; 24 hours) induces BRD4 degradation in LS174t cells 24 h. MZ 1 leads to complete degradation of BRD4 protein, whereas the expression of BRD4 mRNA is not reduced[3].

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[3]

Cell Line: LS174t cells
Concentration: 0, 100, and 250 nM
Incubation Time: 24 hours
Result: Led to complete degradation of BRD4 protein, whereas the expression of BRD4 mRNA was not reduced.

分子量

1002.64

Formula

C49H60ClN9O8S2

CAS 号

1797406-69-9

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 (99.74 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9974 mL 4.9868 mL 9.9737 mL
5 mM 0.1995 mL 0.9974 mL 1.9947 mL
10 mM 0.0997 mL 0.4987 mL 0.9974 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:

——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: ≥ 2.5 mg/mL (2.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.49 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 (2.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.49 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 (2.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.49 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]. Zengerle M, et al. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4. ACS Chem Biol. 2015 Aug 21;10(8):1770-7.

    [2]. Gadd MS, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 May;13(5):514-521.

    [3]. Otto C, et al. Targeting bromodomain-containing protein 4 (BRD4) inhibits MYC expression in colorectal cancer cells. Neoplasia. 2019 Nov;21(11):1110-1120.

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BRD5648(Synonyms: (R)-BRD0705)

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。

BRD5648 (Synonyms: (R)-BRD0705) 纯度: 97.07%

BRD5648 ((R)-BRD0705) 是一种 BRD0705 的 阴性对照,BRD0705 是一种有效的,具有旁系选择性和口服活性的 GSK3α 抑制剂,IC50 为 66 nM,Kd 为 4.8 μM。BRD0705 与 GSK3β (IC50 为 515 nM) 相比,对 GSK3α 的选择性更高 (8 倍)。BRD0705 可用于急性髓细胞性白血病。

BRD5648(Synonyms: (R)-BRD0705)

BRD5648 Chemical Structure

CAS No. : 2056261-42-6

规格 价格 是否有货 数量
5 mg ¥5500 In-stock
10 mg ¥8900 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Orally Active Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Glucose Metabolism Compound Library

生物活性

BRD5648 ((R)-BRD0705) is a negative control of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML)[1][2].

体外研究
(In Vitro)

BRD5648, the inactive enantiomer of BRD0705, does not induce changes in enzyme phosphorylation or total β-catenin protein stabilization[1].

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

分子量

321.42

Formula

C20H23N3O

CAS 号

2056261-42-6

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 : 300 mg/mL (933.36 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1112 mL 15.5560 mL 31.1119 mL
5 mM 0.6222 mL 3.1112 mL 6.2224 mL
10 mM 0.3111 mL 1.5556 mL 3.1112 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。

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: ≥ 7.5 mg/mL (23.33 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (23.33 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 75.0 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

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Wagner FF, et al. Exploiting an Asp-Glu “switch” in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia. Sci Transl Med. 2018 Mar 7;10(431). pii: eaam8460.

    [2]. Wagner FF, et al. Exploiting an Asp-Glu “switch” in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia. Sci Transl Med. 2018 Mar 7;10(431). pii: eaam8460.

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ARV-825

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。

ARV-825  纯度: 99.32%

ARV-825 是由Cereblon配体和BRD4配体相连的PROTAC 。ARV-825 对 BRD4 的 BD1 和 BD2 结构域具有高亲和力,Kd 值分别为 90 和 28 nM。

ARV-825

ARV-825 Chemical Structure

CAS No. : 1818885-28-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2539 In-stock
5 mg ¥1600 In-stock
10 mg ¥2500 In-stock
50 mg ¥8400 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

ARV-825 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
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

ARV-825 is a PROTAC connected by ligands for Cereblon and BRD4. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.

IC50 & Target

Kd: 90 nM (Bromodomain 1 of BRD4), 28 nM (Bromodomain 2 of BRD4)[1]

体外研究
(In Vitro)

ARV-825 is a hetero-bifunctional proteolysis-targeting chimera (PROTAC) that recruits BRD4 to the E3 ubiquitin ligase cereblon. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of the former via the proteasome. Given that BRD4 and cereblon binding moieties in ARV-825 have Kds of 28-90 nM and ~3 µM to their respective targets, this suggests that ARV-825 acts in a substoichiometric way in mediating BRD4 degradation. ARV-825 treatment results in prolonged BRD4 down-regulation and downstream signaling suppression compared to BRD4 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

923.43

Formula

C46H47ClN8O9S

CAS 号

1818885-28-7

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 (54.15 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 1.0829 mL 5.4146 mL 10.8292 mL
5 mM 0.2166 mL 1.0829 mL 2.1658 mL
10 mM 0.1083 mL 0.5415 mL 1.0829 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。

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: ≥ 2.5 mg/mL (2.71 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.71 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% corn oil

    Solubility: ≥ 2.5 mg/mL (2.71 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.71 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]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63.

Kinase Assay
[1]

Affinity of compounds (e.g., ARV-825) with Bromodomain 1 and 2 of BRD4 is determined with BROMOscan by DiscoverX[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]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63.

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dBET1

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。

dBET1  纯度: 98.09%

dBET1 是由Cereblon配体和BRD4配体相连的PROTAC,其 EC50 值为 430 nM。dBET1 是一种由 BRD4 抑制剂 JQ1 (HY-13030) 与 NSC 527179 (HY-14658) 衍生物通过 linker 产生的 PROTAC,能够在低纳摩尔浓度下诱导 BRD4 降解。

dBET1

dBET1 Chemical Structure

CAS No. : 1799711-21-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2380 In-stock
2 mg ¥880 In-stock
5 mg ¥1450 In-stock
10 mg ¥2600 In-stock
25 mg ¥5400 In-stock
50 mg ¥9100 In-stock
100 mg ¥16000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

dBET1 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
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker[1].

IC50 & Target

BRD4

430 nM (EC50)

Cereblon

 

体外研究
(In Vitro)

Treatment with dBET1 down regulates MYC and PIM1 transcription. Degradation of BRD4 by dBET1 is associated with a more potent apoptotic consequence in MV4;11 cell line. Significantly increased apoptosis after only 4 h of dBET1 treatment is enhanced at 8 h. dBET1 also induces a potent and superior inhibitory effect on MV4;11 cell proliferation at 24 hours (measured by ATP content, IC50= 0.14 μM, compare to IC50= 1.1 μM with JQ1)[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)

Administration of dBET1 attenuates tumor progression as determined by serial volumetric measurement, and decreases tumor weight assessed post-mortem. Acute pharmacodynamic degradation of BRD4 is observed four hours after a first or second daily treatment with dBET1 (50 mg/kg IP). A statistically significant destabilization of BRD4, down regulation of MYC and inhibition of proliferation is observed with dBET1 compare to vehicle control in excised tumors. Two weeks of dBET1 is well tolerated by mice without a meaningful effect on weight, white blood count, hematocrit or platelet count[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

785.27

Formula

C38H37ClN8O7S

CAS 号

1799711-21-9

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 : 43.33 mg/mL (55.18 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2734 mL 6.3672 mL 12.7345 mL
5 mM 0.2547 mL 1.2734 mL 2.5469 mL
10 mM 0.1273 mL 0.6367 mL 1.2734 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。

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    90% corn oil

    Solubility: ≥ 3 mg/mL (3.82 mM); Clear solution

    此方案可获得 ≥ 3 mg/mL (3.82 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 30.0 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]. Winter GE, et al. DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science. 2015 Jun 19;348(6241):1376-81.

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-987

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-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

GNE-987 Chemical Structure

CAS No. : 2417371-71-0

规格 价格 是否有货 数量
1 mg ¥5950 In-stock
5 mg ¥13500 In-stock
10 mg ¥21500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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:

——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    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.

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

BRD0705

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。

BRD0705  纯度: 98.41%

BRD0705 是一种有效的,具有旁系选择性和口服活性的 GSK3α 抑制剂,IC50 为 66 nM,Kd 为 4.8 μM。 BRD0705 与 GSK3β (IC50 为 515 nM) 相比,对 GSK3α 的选择性更高 (8 倍)。BRD0705 可用于急性髓细胞性白血病的研究。

BRD0705

BRD0705 Chemical Structure

CAS No. : 2056261-41-5

规格 价格 是否有货 数量
5 mg ¥5500 In-stock
10 mg ¥8900 In-stock
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

BRD0705 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Wnt/Hedgehog/Notch Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Orally Active Compound Library
  • Anti-Alzheimer’s Disease Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Glucose Metabolism Compound Library

生物活性

BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research[1].

IC50 & Target[1]

GSK3α

66 nM (IC50)

GSK3α

4.8 μM (Kd)

GSK-3β(WT)

515 nM (IC50)

体外研究
(In Vitro)

BRD0705 displays excellent selectivity in a penal of 311 kinases, the CDK family of kinases (CDK2, 3 and 5) are next most potently inhibits at values of 6.87 μM, 9.74 μM and 9.20 μM (87-fold, 123-fold and 116-fold selectivity relative to GSK3α)[1].
BRD0705 (10-40 μM; 2-24 hours; U937 cells) treatment impairs GSK3α Tyr279 phosphorylation in a time-and concentration-dependent manner without affecting GSK3β Tyr216 phosphorylation[1].
Using a β-catenin dependent TCF/LEF luciferase reporter assay, the absence of β-catenin induced target activation after treatment with BRD0705 in AML cell lines[1].
BRD0705 impairs AML colony formation in all six tested cell lines, MOLM13, TF-1, U937, MV4-11, HL-60 and NB4, in a concentration-dependent manner, as opposed to BRD3731 which impairs colony formation in TF-1 while increasing colony forming ability in the MV4-11 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.

Western Blot Analysis[1]

Cell Line: U937 cells
Concentration: 10 μM, 20 μM and 40 μM
Incubation Time: 2 hours, 4 hours, 8 hours and 24 hours
Result: Impaired GSK3α Tyr279 phosphorylation in a time-and concentration-dependent manner without affecting GSK3β Tyr216 phosphorylation.

体内研究
(In Vivo)

BRD0705 (30 mg/kg; oral gavage; twice daily; NSG mice) treatment impairs leukemia initiation and prolongs survival in AML mouse models[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 Model: 8-week-old male NSG mice injected with MLL-AF9 AML cells[1]
Dosage: 30 mg/kg
Administration: Oral gavage; twice daily
Result: Mice survival was significantly improved.

分子量

321.42

Formula

C20H23N3O

CAS 号

2056261-41-5

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 : 300 mg/mL (933.36 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1112 mL 15.5560 mL 31.1119 mL
5 mM 0.6222 mL 3.1112 mL 6.2224 mL
10 mM 0.3111 mL 1.5556 mL 3.1112 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。

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: ≥ 7.5 mg/mL (23.33 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (23.33 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 75.0 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% corn oil

    Solubility: ≥ 7.5 mg/mL (23.33 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (23.33 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]. Wagner FF, et al. Exploiting an Asp-Glu “switch” in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia. Sci Transl Med. 2018 Mar 7;10(431). pii: eaam8460.

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

BRD9876

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。

BRD9876  纯度: 98.33%

BRD9876 是一种 “rigor” 抑制剂,可将驱动蛋白 5 (Eg5) 锁定在增强微管 (MTs) 结合的状态,从而导致 MT 的捆绑和稳定。BRD9876 与酪氨酸 104 残基相互作用,该残基是 α4-α6 变构结合口袋的一部分。BRD9876 特异性靶向微管结合的 Eg5,选择性抑制 CD34 细胞的骨髓瘤。BRD9876 具有用于多发性骨髓瘤 (MM) 研究的潜力。

BRD9876

BRD9876 Chemical Structure

CAS No. : 32703-82-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥880 In-stock
50 mg ¥800 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

BRD9876 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Cytoskeleton Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research[1][2][3][4].

体外研究
(In Vitro)

BRD9876 (10 μM; 24 hours) reveales rapid arrest of cells at the G2/M phase starting as early as 2h of treatment in MM1S cells[1].
BRD9876 exhibits approximately 3-fold selectivity for MM1S myeloma cells (IC50=3.1 μM) over CD34+ derived hematopoietic cells (IC50=9.1 μM)[1].
BRD9876 (0.1, 1, 10, 100 uM) is able to overcome, in MM1S cells, stromal resistance of bone marrow stromal cells (BMSCs) from MM bone marrow aspirates but only minimal effects are observed with BRD9876 against primary MM cells[1].
BRD9876 is completely ineffective at inhibiting the basal ATPase activity of Eg5, in contrast to loop L5-binding monastrol or α4/α6-binding BI8 which shows greater activity against basal Eg5 ATPase activity[1].

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

Cell Cycle Analysis[1]

Cell Line: MM1S cells and CD34 hematopoietic cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: Revealed rapid arrest of cells at the G2/M phase starting as early as 2h of treatment in MM1S cells.
Showed markedly less G2/M arrest in CD34 hematopoietic cells.

分子量

234.30

Formula

C16H14N2

CAS 号

32703-82-5

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 : 50 mg/mL (213.40 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.2680 mL 21.3402 mL 42.6803 mL
5 mM 0.8536 mL 4.2680 mL 8.5361 mL
10 mM 0.4268 mL 2.1340 mL 4.2680 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:

——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    90% corn oil

    Solubility: ≥ 2.5 mg/mL (10.67 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.67 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Shrikanta Chattopadhyay, et al. Niche-Based Screening in Multiple Myeloma Identifies a Kinesin-5 Inhibitor with Improved Selectivity over Hematopoietic Progenitors. Cell Rep. 2015 Feb 10;10(5):755-770.

    [2]. Chieh-Ting Fang, et al. HSP70 regulates Eg5 distribution within the mitotic spindle and modulates the cytotoxicity of Eg5 inhibitors. Cell Death Dis. 2020 Sep 1;11(8):715.

    [3]. Anke Maes, et al. The therapeutic potential of cell cycle targeting in multiple myeloma. Oncotarget. 2017 Jun 28;8(52):90501-90520.

    [4]. Geng-Yuan Chen, et al. Eg5 Inhibitors Have Contrasting Effects on Microtubule Stability and Metaphase Spindle Integrity. ACS Chem Biol. 2017 Apr 21;12(4):1038-1046.

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

BRD4770

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。

BRD4770  纯度: 99.77%

BRD4770 是一种组蛋白甲基转移酶 G9a 抑制剂。BRD4770 可抑制 H3K9 的二甲基和三甲基化,EC50 为 5 µM,对 H3K27me3,H3K36me3,H3K4me3 和 H3K79me3 几乎没有影响。BRD4770 可以激活共济失调毛细血管扩张突变 (ATM) 途径并诱导细胞衰老。

BRD4770

BRD4770 Chemical Structure

CAS No. : 1374601-40-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1430 In-stock
10 mg ¥1300 In-stock
50 mg ¥4200 In-stock
100 mg ¥7500 In-stock
500 mg ¥13500 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

BRD4770 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
  • Reprogramming Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 µM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence[1].

IC50 & Target

Histone methyltransferase G9a[1]

体外研究
(In Vitro)

BRD4770 (0-20 µM; 72 hours; PANC-1 cells) treatment reduces the number of cells after 72 h[1].
BRD4770 (2.5-5 µM; 24 hours; PANC-1 cells) treatment decreases H3K9 trimethylation level by 23% in PANC-1 cells[1].
BRD4770 induces a senescent phenotype in a pancreatic cancer cell line. BRD4770 also inhibits both anchorage-dependent and -independent cell proliferation and induces G2/M cell-cycle arrest. BRD4770 activates the ataxia telangiectasia mutated (ATM) pathway without inducing DNA damage, while the ataxia telangiectasia and Rad3-related protein (ATR) pathway is not affected[1].
BRD4770 also induces increased levels of lysine acetylation in cells without inhibiting histone deacetylases[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 Viability Assay[1]

Cell Line: PANC-1 cells
Concentration: 0 µM, 0.625 µM, 1.25 µM, 2.5 µM, 5 µM, 10 µM, 20 µM
Incubation Time: 72 hours
Result: Reduced the number of cells after 72 h.

Western Blot Analysis[1]

Cell Line: PANC-1 cells
Concentration: 2.5 µM, 5 µM
Incubation Time: 24 hours
Result: Decreased H3K9 trimethylation level by 23% in PANC-1 cells.

分子量

413.47

Formula

C25H23N3O3

CAS 号

1374601-40-7

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 : 33.33 mg/mL (80.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4186 mL 12.0928 mL 24.1856 mL
5 mM 0.4837 mL 2.4186 mL 4.8371 mL
10 mM 0.2419 mL 1.2093 mL 2.4186 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。

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: 0.5% Methylcellulose/saline water

    Solubility: 6.25 mg/mL (15.12 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.05 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]. Yuan Y, et al. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem Biol. 2012 Jul 20;7(7):1152-7.

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

PROTAC BRD9 Degrader-1

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。

PROTAC BRD9 Degrader-1  纯度: 98.30%

PROTAC BRD9 Degrader-1 是一种由Cereblon配体和BRD9配体相连的PROTAC,可用作研究 BAF 复合物的选择性探针。

PROTAC BRD9 Degrader-1

PROTAC BRD9 Degrader-1 Chemical Structure

CAS No. : 2097971-01-0

规格 价格 是否有货 数量
5 mg ¥11000 In-stock
10 mg ¥17000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

PROTAC BRD9 Degrader-1 相关产品

相关化合物库:

  • Bioactive Compound Library Plus

生物活性

PROTAC BRD9 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD9 (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology[1].

IC50 & Target[1]

BRD9

13.5 nM (IC50)

BRD4

3.78 μM (IC50)

CRBN-DDB1

48.9 nM (IC50)

体外研究
(In Vitro)

PROTAC BRD9 Degrader-1 (Compound 1) inhibits BRD9, BRD4, and CRBN-DDB1 with IC50s of 13.5 nM, 3.78 μM, and 48.9 nM, 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

903.98

Formula

C42H45N7O12S2

CAS 号

2097971-01-0

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 (165.93 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1062 mL 5.5311 mL 11.0622 mL
5 mM 0.2212 mL 1.1062 mL 2.2124 mL
10 mM 0.1106 mL 0.5531 mL 1.1062 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:

——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: ≥ 2.5 mg/mL (2.77 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.77 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 (2.77 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.77 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
*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]. Remillard D, et al. Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands. Angew Chem Int Ed Engl. 2017 May 15;56(21):5738-5743.

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

PROTAC BRD4 Degrader-1

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。

PROTAC BRD4 Degrader-1 

PROTAC BRD4 Degrader-1 是由Cereblon配体和BRD4配体相连的PROTAC,抑制 BRD4 BD1 的 IC50 为 41.8 nM。PROTAC BRD4 Degrader-1 可以有效降解 BRD4 蛋白并抑制 c-Myc 表达。

PROTAC BRD4 Degrader-1

PROTAC BRD4 Degrader-1 Chemical Structure

CAS No. : 2133360-00-4

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生物活性

PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression[1].

IC50 & Target

BRD4 (BD1)

41.8 nM (IC50)

体外研究
(In Vitro)

PROTAC BRD4 Degrader-1 (compound 21) (2.5 μM; 24 hours) shows high inhibitory activity against the growth of human monocyte lymphoma cell line THP-1, with the IC50 value of 0.81 μM, and moderate activity against Raji and HL-60 cell lines[1].
PROTAC BRD4 Degrader-1 (1 μM; 24 hours) effectively induces the degradation of BRD4 protein and suppression of c-Myc, while pomalidomide couldn’t degrade BRD4 at the low concentration[1].

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

Cell Proliferation Assay[1]

Cell Line: HL-60, Raji and THP-1 cell
Concentration: 2.5 μM
Incubation Time: 24 hours
Result: Inhibited HL-60, Raji and THP-1 cell growth.

Western Blot Analysis[1]

Cell Line: THP-1 cell
Concentration: 1 μM
Incubation Time: 3 hours
Result: Degraded BRD4 protein and suppressed c-Myc expression.

分子量

771.78

Formula

C40H37N9O8

CAS 号

2133360-00-4

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]. Zhang F, et al. Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide.Bioorg Med Chem. 2020 Jan 1;28(1):115228.

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PROTAC BRD4 Degrader-3

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。

PROTAC BRD4 Degrader-3 

PROTAC BRD4 Degrader-3 (compound 1004.1) 是一种有效的由von Hippel-Lindau配体和BRD4配体相连的PROTAC 。

PROTAC BRD4 Degrader-3

PROTAC BRD4 Degrader-3 Chemical Structure

CAS No. : 2313234-00-1

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生物活性

PROTAC BRD4 Degrader-3 (compound 1004.1) is an efficacious PROTAC connected by ligands for von Hippel-Lindau and BRD4[1].

IC50 & Target[1]

BRD4

 

分子量

1098.29

Formula

C55H65F2N9O9S2

CAS 号

2313234-00-1

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]. Peter Dragovich, et al. (4-hydroxypyrrolidin-2-yl)-hydroxamate compounds and methods of use thereof. WO2019084030A1.

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BRD-IN-3

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。

BRD-IN-3 

BRD-IN-3 ((R,R)-36n) 是一个强效的P300/CBP 相关因子溴端结构域 (PCAF BRD) 的抑制剂,其IC50 值为 7 nM。BRD-IN-3 也能抑制GCN5 和FALZ。

BRD-IN-3

BRD-IN-3 Chemical Structure

CAS No. : 2351938-32-2

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生物活性

BRD-IN-3 ((R,R)-36n) is a highly potent PCAF bromodomain (BRD) inhibitor, with an IC50 of 7 nM. BRD-IN-3 also exhibits activity against GCN5 and FALZ[1].

IC50 & Target

IC50: PCAF BRD[1].

分子量

395.45

Formula

C21H25N5O3

CAS 号

2351938-32-2

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]. Huang L, et al. Discovery of Pyrrolo[3,2- d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain. J Med Chem. 2019 May 9;62(9):4526-4542.

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PROTAC BRD4 Degrader-2

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。

PROTAC BRD4 Degrader-2 

PROTAC BRD4 Degrader-2 是由Cereblon配体和BRD4配体相连的PROTAC,对 BRD4 BD1IC50 为 14.2 nM。

PROTAC BRD4 Degrader-2

PROTAC BRD4 Degrader-2 Chemical Structure

CAS No. : 2185795-53-1

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250 mg   询价  
500 mg   询价  

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生物活性

PROTAC BRD4 Degrader-2 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 14.2 nM against BRD4 BD1[1].

IC50 & Target[1]

BRD4 BD1

14.2 nM (IC50)

Cereblon

 

体外研究
(In Vitro)

PROTAC BRD4 Degrader-2 (Compound 17) inhibits the growth of THP-1 cell line with an IC50 of 1.83±0.016 μM[1].

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

Cell Proliferation Assay[1]

Cell Line: Human monocyte lymphoma cell line THP-1
Concentration: 72 hours
Incubation Time: 0.81-3.26 μM
Result: Showd high anti-proliferative potency.

分子量

757.79

Formula

C40H39N9O7

CAS 号

2185795-53-1

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]. Zhang F, et al. Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228.

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PROTAC BRD4 Degrader-7

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。

PROTAC BRD4 Degrader-7 

PROTAC BRD4 Degrader-7 是一种有效的溴结构域 BRD4 降解剂,对 BRD4-BD1 和 BRD4-BD2 的 IC50 分别为 15.5 和 12.3 nM。详细信息请参见专利 WO2020055976A1,example 1a。

PROTAC BRD4 Degrader-7

PROTAC BRD4 Degrader-7 Chemical Structure

CAS No. : 2413382-30-4

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生物活性

PROTAC BRD4 Degrader-7 is a potent bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC50s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively[1].

IC50 & Target[1]

BRD4 BD1

15.5 nM (IC50)

BRD4 BD2

12.3 nM (IC50)

体外研究
(In Vitro)

PROTAC BRD4 Degrader-7 shows an IC50 of 27.1 nM in BRD4 Full Length Binding assay. PROTAC BRD4 Degrader-7 degrades BRD4 with an EC50 of 1.4 nM for PC3-Steapl cells and an IC50 of 1.3 nM for EoL-1 Cells. PROTAC BRD4 Degrader-7 inhibits PC-3-STEAP-1 and EoL-l proliferation with IC50s of 6.6 and 2.2 nM, respectively. PROTAC BRD4 Degrader-7 inhibits MYC expression in MV-4-11 cells with an IC50 of 2.9 nM[1].

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

分子量

475.61

Formula

C26H29N5O2S

CAS 号

2413382-30-4

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]. Robert Anthony BLAKE, et al. Tert-butyl (s)-2-(4-(phenyl)-6h-thieno[3,2-f][1,2,4]triazolo[4,3-a] [1,4]diazepin-6-yl) acetate derivatives and related compounds as bromodomain brd4 inhibitors for treating cancer. WO2020055976A1.

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