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.
IC50&Target
IC50: 29 nM (RIP1 in FP binding assay).
体外研究
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.
体内研究
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.
Animal Model:
C57BL/6 mice.
Dosage:
0.2 mg/kg, 2 mg/kg, 10 mg/kg.
Administration:
IP once.
Result:
Protected mice from TNF+zVAD-induced hypothermia.
分子式
C14H18N2O
分子量
230.31
CAS号
2049868-46-2
运输条件
Room temperature in continental US; may vary elsewhere.