JNK-IN-8 | CAS:1410880-22-6

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Name:JNK-IN-8; 
Cat. No. :CS-0601
CAS No. :1410880-22-6
Formula:C29H29N7O2
M. Wt. : 507.59
Solubility:DMSO: ≥ 35 mg/mL

JNK-IN-8 is a potent JNK inhibitor with IC50 of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively. IC50 & Target: IC50: 4.7/18.7/1 nM (JNK1/2/3)[1]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[1]. 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[2].

Zhang T, et al. Discovery of potent and selective covalent inhibitors of JNK. Chem Biol. 2012 Jan 27;19(1):140-54. Liu Q, et al. Developing irreversible inhibitors of the protein kinase cysteinome. Chem Biol. 2013 Feb 21;20(2):146-59.