MLKL activator 1

发表于2024年11月14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。

RIP1/RIP3/MLKL activator 1

RIP1/RIP3/MLKL activator 1 (Compound 6i) 是一种有效的抗胶质瘤 (anti-glioma) 药物。RIP1/RIP3/MLKL activator 1 通过激活 RIP1/RIP3/MLKL 通路诱导细胞坏死（necroptosis）。 RIP1/RIP3/MLKL activator 1 可透过血脑屏障。

RIP1/RIP3/MLKL activator 1 Chemical Structure

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

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生物活性

RIP1/RIP3/MLKL activator 1 (Compound 6i) is a potent anti-glioma agent. RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway. RIP1/RIP3/MLKL activator 1 exerts acceptable BBB permeability^[1].

IC₅₀ & Target

RIP1, RIP3, MLKL^[1]

体外研究
(In Vitro)

RIP1/RIP3/MLKL activator 1 (Compound 6i) (96 h) shows antiproliferative activities in human glioma cell lines^[1].
RIP1/RIP3/MLKL activator 1 (0-4 µM, 0-72 h) exhibits remarkable antiproliferative activity for U251 cells in a time- and concentration-dependent manner^[1].
RIP1/RIP3/MLKL activator 1 (10 µM, 0-72 h) shows acceptable stability^[1].
RIP1/RIP3/MLKL activator 1 (0-2 µM, 24 h) effectively inhibits the migration of U251 cells^[1].
RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway, and induces mitochondrial depolarization in U251 cells^[1].
RIP1/RIP3/MLKL activator 1 could not induce apoptosis in U251 cells^[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:	A172, LN229, U87, U251 and L02 cell lines
Concentration:	0-4 µM for U251 cells
Incubation Time:	96 h; 24, 48, and 72 h for U251 cells
Result:	Showed antiproliferative activity with IC₅₀ values of 3.03 ± 0.70, 1.78 ± 0.79, 1.22 ± 0.89, 0.94 ± 0.45, and 0.99 ± 0.46 µM against A172, LN229, U87, U251 and L02 cells, respectively. Time- and concentration-dependently inhibited the growth in U251 cells.

Western Blot Analysis^[1]

Cell Line:	U251
Concentration:	0, 0.5, 1, 2, and 4 µM
Incubation Time:	24 or 48 h
Result:	Concentration-dependently upregulated the expression of p-RIP1, RIP1, p-RIP3, RIP3, p-MLKL, and MLKL at 24 or 48 h.

体内研究
(In Vivo)

RIP1/RIP3/MLKL activator 1 (Compound 6i) (2.50 ng/tail; i.v.; 48 h) inhibits U251 cell proliferation in vivo and exerts acceptable BBB permeability^[1].

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

Animal Model:	Zebrafish wide-type AB strain; 200 CM-DiI labeled U251 cells were transplanted into yolk sac of each wild-type zebrafish embryos at 2 dpf (2 days postfertilization)^[1]
Dosage:	2.50 ng/tail
Administration:	Microinjection; 48 h
Result:	Remarkably reduced the U251 xenografts fluorescence intensity.

分子量

676.93

Formula

C₄₃H₅₆N₄O₃

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]. Yao Feng, et al. Synthesis and biological evaluation of celastrol derivatives as potential anti-glioma agents by activating RIP1/RIP3/MLKL pathway to induce necroptosis. Eur J Med Chem. 2022 Feb 5;229:114070.

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

RIP1/RIP3/MLKL activator 1

发表于2024年11月13日由上海金畔生物科技有限公司

RIP1/RIP3/MLKL activator 1

RIP1/RIP3/MLKL activator 1 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

IC₅₀ & Target

RIP1, RIP3, MLKL^[1]

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.

Cell Proliferation Assay^[1]

Cell Line:	A172, LN229, U87, U251 and L02 cell lines
Concentration:	0-4 µM for U251 cells
Incubation Time:	96 h; 24, 48, and 72 h for U251 cells
Result:	Showed antiproliferative activity with IC₅₀ values of 3.03 ± 0.70, 1.78 ± 0.79, 1.22 ± 0.89, 0.94 ± 0.45, and 0.99 ± 0.46 µM against A172, LN229, U87, U251 and L02 cells, respectively. Time- and concentration-dependently inhibited the growth in U251 cells.

Western Blot Analysis^[1]

Cell Line:	U251
Concentration:	0, 0.5, 1, 2, and 4 µM
Incubation Time:	24 or 48 h
Result:	Concentration-dependently upregulated the expression of p-RIP1, RIP1, p-RIP3, RIP3, p-MLKL, and MLKL at 24 or 48 h.

体内研究
(In Vivo)

RIP1/RIP3/MLKL activator 1 (Compound 6i) (2.50 ng/tail; i.v.; 48 h) inhibits U251 cell proliferation in vivo and exerts acceptable BBB permeability^[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:	Zebrafish wide-type AB strain; 200 CM-DiI labeled U251 cells were transplanted into yolk sac of each wild-type zebrafish embryos at 2 dpf (2 days postfertilization)^[1]
Dosage:	2.50 ng/tail
Administration:	Microinjection; 48 h
Result:	Remarkably reduced the U251 xenografts fluorescence intensity.

分子量

676.93

Formula

C₄₃H₅₆N₄O₃

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]. Yao Feng, et al. Synthesis and biological evaluation of celastrol derivatives as potential anti-glioma agents by activating RIP1/RIP3/MLKL pathway to induce necroptosis. Eur J Med Chem. 2022 Feb 5;229:114070.

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

RIP1/RIP3/MLKL activator 1

发表于2024年11月13日由上海金畔生物科技有限公司

RIP1/RIP3/MLKL activator 1

RIP1/RIP3/MLKL activator 1 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

IC₅₀ & Target

RIP1, RIP3, MLKL^[1]

体外研究
(In Vitro)

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:	A172, LN229, U87, U251 and L02 cell lines
Concentration:	0-4 µM for U251 cells
Incubation Time:	96 h; 24, 48, and 72 h for U251 cells
Result:	Showed antiproliferative activity with IC₅₀ values of 3.03 ± 0.70, 1.78 ± 0.79, 1.22 ± 0.89, 0.94 ± 0.45, and 0.99 ± 0.46 µM against A172, LN229, U87, U251 and L02 cells, respectively. Time- and concentration-dependently inhibited the growth in U251 cells.

Western Blot Analysis^[1]

Cell Line:	U251
Concentration:	0, 0.5, 1, 2, and 4 µM
Incubation Time:	24 or 48 h
Result:	Concentration-dependently upregulated the expression of p-RIP1, RIP1, p-RIP3, RIP3, p-MLKL, and MLKL at 24 or 48 h.

体内研究
(In Vivo)

RIP1/RIP3/MLKL activator 1 (Compound 6i) (2.50 ng/tail; i.v.; 48 h) inhibits U251 cell proliferation in vivo and exerts acceptable BBB permeability^[1].

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

Animal Model:	Zebrafish wide-type AB strain; 200 CM-DiI labeled U251 cells were transplanted into yolk sac of each wild-type zebrafish embryos at 2 dpf (2 days postfertilization)^[1]
Dosage:	2.50 ng/tail
Administration:	Microinjection; 48 h
Result:	Remarkably reduced the U251 xenografts fluorescence intensity.

分子量

676.93

Formula

C₄₃H₅₆N₄O₃

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]. Yao Feng, et al. Synthesis and biological evaluation of celastrol derivatives as potential anti-glioma agents by activating RIP1/RIP3/MLKL pathway to induce necroptosis. Eur J Med Chem. 2022 Feb 5;229:114070.

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

Necrosulfonamide

发表于2024年10月23日由上海金畔生物科技有限公司

Necrosulfonamide 纯度: 98.19%

Necrosulfonamide，一种 necroptosis 抑制剂，通过选择性靶向 (MLKL)。Necrosulfonamide 阻止 MLKL-RIP1-RIP3 坏死小体复合体与其下游效应子相互作用。MLKL 是诱导坏死过程中 RIP3 的重要底物。

Necrosulfonamide Chemical Structure

CAS No. : 1360614-48-7

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥660	In-stock
5 mg	￥600	In-stock
10 mg	￥770	In-stock
25 mg	￥1500	In-stock
50 mg	￥2200	In-stock
100 mg	￥4000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Necrosulfonamide 相关产品

•相关化合物库:

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

生物活性

Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis^[1].

体外研究
(In Vitro)

Necrosulfonamide specifically blocks necrosis downstream of RIP3 activation. Necrosulfonamide inhibits MLKL-mediated necrosis by blocking Its N-terminal CC domain function^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

461.47

Formula

C₁₈H₁₅N₅O₆S₂

CAS 号

1360614-48-7

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 : ≥ 28 mg/mL (60.68 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	2.1670 mL	10.8349 mL	21.6699 mL
5 mM	0.4334 mL	2.1670 mL	4.3340 mL
10 mM	0.2167 mL	1.0835 mL	2.1670 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： 50% PEG300 50% saline

Solubility: 10 mg/mL (21.67 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 20% SBE-β-CD in saline

Solubility: 6.67 mg/mL (14.45 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: 2.5 mg/mL (5.42 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.42 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 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: 2.5 mg/mL (5.42 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.42 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
5.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: 2.5 mg/mL (5.42 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.42 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玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。

参考文献

[1]. Sun L, et al. Mixed lineage kinase domain-like protein mediates necrosis signaling downstream of RIP3 kinase. Cell. 2012;148(1-2):213-227.

RIP2 kinase inhibitor 2

发表于2024年4月28日由上海金畔生物科技有限公司

RIP2 kinase inhibitor 2 纯度: 99.16%

RIP2 kinase inhibitor 2 是一种受体相互作用蛋白-2 (RIP2) 激酶抑制剂，详细信息请参考专利 WO/2014043437 A1 中的化合物 example 9。

RIP2 kinase inhibitor 2 Chemical Structure

CAS No. : 1581270-11-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3331	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.

RIP2 kinase inhibitor 2 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Kinase Inhibitor Library
NF-κB Signaling Compound Library
Anti-Cancer Compound Library

生物活性

RIP2 kinase inhibitor 2 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043437 A1, compound example 9.

IC₅₀ & Target

RIP2 Kinase^[1]

体外研究
(In Vitro)

RIP2 kinase inhibitor 2 is a novel prodrug of a quinazolyl amine that inhibits RIP2 kinase. Receptor interacting protein-2 (RIP2) kinase is a TKL family serine/threonine protein kinase involved in innate immune signaling. Following activation, RIP2 kinase associates with NODI or NOD2 and appears to function principally as a molecular scaffold to bring together other kinases (TAK1, ΙΚΚα/β/γ) involved in NF-κΒ and mitogen-activated protein kinase activation^[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

432.54

Formula

C₂₁H₂₈N₄O₄S

CAS 号

1581270-11-2

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 : 5 mg/mL (11.56 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3119 mL	11.5596 mL	23.1192 mL
5 mM	0.4624 mL	2.3119 mL	4.6238 mL
10 mM	0.2312 mL	1.1560 mL	2.3119 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: ≥ 0.5 mg/mL (1.16 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (1.16 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 5.0 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: ≥ 0.5 mg/mL (1.16 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (1.16 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 5.0 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: ≥ 0.5 mg/mL (1.16 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (1.16 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 5.0 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]. Linda N. Casillas, et al. Amino-quinolines as kinase inhibitors. PCT Int. Appl. (2014), WO 2014043437 A1 20140320.

Animal Administration ^[1]	Rats^[1] Rats are orally pre-dosed with the RIP2 kinase inhibitor 2, at doses of 0.016, 0.16 and 1.6 mg/kg (n=8 rats/group), followed by dosing with L18-MDP (50 μg/rat) 0.25 hours after pre-dosing with the compound. The IL8 cytokine levels and percentage levels are calculated as the mean±standard error of the mean (n=8 rats/group). 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]. Linda N. Casillas, et al. Amino-quinolines as kinase inhibitors. PCT Int. Appl. (2014), WO 2014043437 A1 20140320.

Animal Administration
^[1]

Rats^[1]
Rats are orally pre-dosed with the RIP2 kinase inhibitor 2, at doses of 0.016, 0.16 and 1.6 mg/kg (n=8 rats/group), followed by dosing with L18-MDP (50 μg/rat) 0.25 hours after pre-dosing with the compound. The IL8 cytokine levels and percentage levels are calculated as the mean±standard error of the mean (n=8 rats/group).

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]. Linda N. Casillas, et al. Amino-quinolines as kinase inhibitors. PCT Int. Appl. (2014), WO 2014043437 A1 20140320.

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

whatman (沃特曼)

英国沃特曼 Millipore PALL中国代理商金畔官网

标签归档：rip

RIP1/RIP3/MLKL activator 1

RIP1/RIP3/MLKL activator 1

RIP1/RIP3/MLKL activator 1

Necrosulfonamide

Necrosulfonamide 相关产品

•相关化合物库:

RIP2 kinase inhibitor 2

RIP2 kinase inhibitor 2 相关产品

•相关化合物库:

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