GSK963 是一种手性的、强效的、选择性的受体相互作用蛋白 1 (RIP1) 酶的抑制剂，其 IC50 值为 29 nM。GSK963 对体外小鼠和人细胞的坏死具有强效和选择性的抑制作用。
货号:ajcx38620
CAS:2049868-46-2
分子式:C14H18N2O
分子量：230.31
溶解度:DMSO : 25 mg/mL (108.55 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro[1].

GSK963 is >10 000-fold selective for RIP1 over 339 other kinases, lacks measurable activity against IDO and has an inactive enantiomer, GSK962, which can be used to confirm on-target effects[1].

GSK963 (2 mg/kg) results in a complete protection from TNF+zVAD-induced temperature loss. GSK963 (0.2 mg/kg) also shows a significant response[1].

[1]. Berger SB, et al. Characterization of GSK'963: a structurally distinct, potent and selective inhibitor of RIP1 kinase. Cell Death Discov. 2015 Jul 27;1:15009.