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抑制剂描述:

产品名称:GSK-872

产品别名:见爱必信官网

英文别名:GSK-872

靶点:Ser/Thr Protease

CAS:1346546-69-7

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

GSK-872  is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.

溶解性:DMSO : 71 mg/mL (185.1 mM)
Ethanol : 38 mg/mL (99.1 mM)

体外研究:

GSK872 (1 μM) has no inhibition for most of 300 human protein kinases tested. It fails to inhibit RIP1 kinase. In HT-29 cells, GSK872 concentration-dependently blocks TNF-induced necroptosis. In cell-based assays, there is a 100- to 1000-fold shift in the IC50 compared to the cell-free biochemical assays. GSK872 inhibits DAI- or TLR3-induced (RIP1-independent) death. It induces caspase activation and then induces apoptotic cell death.

体内研究:In compared with no treatment after ischemic injury in vivo, GSK872 can significantly reduce HIF-1α expression.

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