JNK-IN-8

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Chemical Structure| 1410880-22-6 同义名 : JNK Inhibitor XVI; c-Jun N-terminal Kinase Inhibitor XVI
CAS号 : 1410880-22-6
货号 : A206353
分子式 : C29H29N7O2
纯度 : 99%+
分子量 : 507.59
MDL号 : MFCD22124890
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(68.95 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • JNK1

    JNK1, IC50:4.7 nM

  • JNK2

    JNK2, IC50:18.7 nM

  • JNK3

    JNK3, IC50:1 nM
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
细胞系 浓度 检测类型 检测时间 活性说明 数据源
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
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.85mL

1.97mL

0.99mL

19.70mL

3.94mL

1.97mL
参考文献

[1]19(1):140-154. doi:10.1016/j.chembiol.2011.11.010

[2]5(8):e129905. doi:10.1172/jci.insight.129905