JNK-IN-8

¥800.00¥1,380.00

SKU: MB4049 分类: , 标签:

JNK-IN-8

分子式:C29H29N7O2分子量:507.59

产品描述

JNK-IN-8是第一个,不可逆JNK抑制剂,作用于JNK1, JNK2和JNK4,IC50分别为4.7 nM, 18.7 nM和1 nM,比作用于MNK2, Fms选择性高10倍以上,对c-Kit, Met, PDGFRβ没有抑制作用。

靶点

JNK3 JNK1 JNK2 Kit (V559D,T670I) Kit (V559D)

IC50

1 nM 4.7 nM 18.7 nM 56 nM 92 nM

体外研究

JNK-IN-8 inhibits c-Jun phosphorylation in HeLa and A375 cells with EC50 of 486 nM and 338 nM, respectively. JNK-IN-8 shows a dramatic improvement in selectivity and eliminated binding to IRAK1, PIK3C3, PIP4K2C, and PIP5K3. JNK-IN-8 requires Cys116 for JNK2 inhibition.JNK-IN-8 (10 mM) suppresses the IL-1β-stimulated phosphorylation of c-Jun in IL-1R cells, an established substrate of the JNKs. JNK-IN-8 covalently attaches to the JNK isoforms caused a small retardation in the electrophoretic mobility of the JNK isoforms.JNK-IN-8 is discovered to inhibit JNK kinase by broad-based kinase selectivity profiling of a library of acrylamide kinase inhibitors based on the structure of imatinib using the KinomeScan approach. JNK-IN-8 possesses distinct regiochemistry of the 1,4-dianiline and 1,3-aminobenzoic acid substructures relative to imatinib and uses an N,N-dimethyl butenoic acetamide warhead to covalently target Cys154. JNK-IN-8 adopts an L-shaped type I binding conformation to access Cys 154 located toward the lip of the ATP-binding site.

体内研究

溶解性

可溶于DMSO

稳定性

2年-20°C粉状,6月-80°C溶于DMSO

特征

运输条件:2~8℃运输

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规格

25mg, 5mg

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