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CAS No.: 1410880-22-6

JNK-IN-8 Catalog No. CSN17808

Synonyms: JNK Inhibitor XVI;c-Jun N-terminal Kinase Inhibitor XVI

JNK-IN-8 is a potent, selective and irreversible JNK inhibitor with IC50 values of 4.7 nM, 18.7 nM and 1 nM for JNK1, 2 and 3, respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 JNK1

IC50:4.67nM JNK2

IC50:18.7nM JNK3

IC50:0.98nM
描述c-Jun N-terminal kinases (JNK1/2/3) are key enzymes in the inflammatory signaling network. JNK-IN-8 is a covalent JNK inhibitor with IC50 values of 4.67, 18.7, and 0.98 nM for JNK1, JNK2, and JNK3, respectively. The EC50 values of JNK-IN-8 for the inhibition of c-Jun phosphorylation in Hela and A375 cells are 486 and 338 nM, respectively. JNK-IN-8 possessed a selective S (10) score of 0.031^[3]. In P411-T1 patient-derived xenograft-derived cells, treatment with 1μM JNK-IN-8 for 24 h led to a significant decrease in p-JUN. JNK-IN-8 at 1 μM also enhanced the inhibitory effect of FOLFOX chemotherapy on cell growth and reversed FOLFOX-induced JUN activation in P441-T1, P442-T1, CFPAC-1, and MIA PaCa-2 cells. In mice bearing pancreatic ductal adenocarcinoma tumors, JNK-IN-8 (30 mg/kg, 2×/week) enhanced the efficacy of FOLFOX chemotherapy on tumor growth^[4].
作用机制JNK-IN-8 inhibits the kinase activity of JNK through the medication of a conserved cysteine in its ATP-binding motif^[3].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human A375 cells	-	Function assay	1 h	Inhibition of JNK3-mediated c-jun phosphorylation in human A375 cells after 1 hr incubation, IC50=0.338 μM	25415535
human HeLa cells	-	Function assay	1 h	Inhibition of JNK3-mediated c-jun phosphorylation in human HeLa cells after 1 hr incubation, IC50=0.486 μM	25415535

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9701 mL
- 9.8505 mL
- 19.7011 mL
- 5 mM
- 0.3940 mL
- 1.9701 mL
- 3.9402 mL
- 10 mM
- 0.1970 mL
- 0.9851 mL
- 1.9701 mL

技术信息

CAS号

1410880-22-6

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H29N7O2

运输

蓝冰

分子量

507.59

别名

JNK Inhibitor XVI;c-Jun N-terminal Kinase Inhibitor XVI

溶解度

DMSO	95.0 mg/mL (187.2 mM) warming
Water	Insoluble
Ethanol	Insoluble

动物实验配方

2% DMSO+30% PEG 300+5% Tween 80+water

10 mg/mL

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靶点	Description	IC50
JNK1		IC50:4.67nM
JNK2		IC50:18.7nM
JNK3		IC50:0.98nM

JNK-IN-8 Catalog No. CSN17808

靶点选择性

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