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CAS No. : 1410880-22-6
MCE 国际站:JNK-IN-8
产品活性:JNK-IN-8 (JNK Inhibitor XVI) 是一种有效的 JNK 抑制剂,抑制 JNK1,JNK2 和 JNK3,IC50 分别为 4.7 nM,18.7 nM 和 1 nM。
研究领域:MAPK/ERK Pathway
作用靶点:JNK
In Vitro: JNK-IN-8 inhibits phosphorylation of c-Jun, a direct substrate of JNK kinase. JNK-IN-8 inhibits c-Jun phosphorylation in HeLa and A375 cells with EC50 of 486 nM and 338 nM, respectively. JNK-IN-8 also exhibits exceptional selectivity based upon KinomeScan and enzymatic profiling. Cumulatively these combined profiling technologies demonstrate that both JNK-IN-8 and JNK-IN-12 are remarkably selective covalent JNK inhibitors and are appropriate for interrogating JNK-dependent biological phenomena.JNK-IN-8, a selective pan-JNK inhibitor, is discovered to inhibit JNK kinase by broad-base kinase selectivity profiling of a library of acrylamide kinase inhibitors based on the structure of imatinib using the KinomeSca approach. JNK-IN-8 possess distinct regio-chemistry of the 1,4-dianiline and 1,3-aminobenzoic acid substructures relative to imatinib and uses an N,N-dimethyl butenoic actemide warhead to covalently target Cys154. JNK-IN-8 adopts an L-shaped type I binding conformation to access Cys 154 located towards the lip of the ATP-binding site.
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