PK68 RIPK1 inhibitor RGNCY-0103
Per 10 mg
PK68 is an inhibitor of RIPK1-dependent necroptosis with an EC50 of 14-22 nM in human and mouse cells. Upon necroptosis stimuli, PK68 significantly blocks the cellular activation of RIPK1 (with selectivity), RIPK3 and MLKL and has favorable pharmacokinetic properties. Significantly, PK68 demonstrates strong protection against TNF-a-induced systemic inflammatory response syndrome in vivo. In addition,PK68 pre-treatment markedly represses metastasis of both melanoma and lung carcinoma cells in mice. PK68 is a potent and selective inhibitor of RIPK1 and demonstrates potential for the treatment of inflammatory disorders and cancer metastasis.
Systematic Name: cyclohexyl (5-(2-acetamidobenzo[d]thiazol-6-yl)-2-methylpyridin-3-yl)carbamate
Mol Wt: 424.52
Discovery of potent necroptosis inhibitors targeting RIPK1 kinase activity for the treatment of inflammatory disorder and cancer metastasis. Hou J et al. Cell Death and Disease (2019) 10:493.
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