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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