GSK872 是一种有效且特异性的 RIP3 激酶抑制剂，降低 RIPK3 介导的坏死和随后的 HMGB1 的细胞质易位和表达，可改善早期脑损伤中的脑水肿和神经功能缺损。它以高亲和力结合 RIP3 激酶结构域，IC50为1.8 nM，并抑制激酶活性，IC50为1.3 nM。

GSK872 (GSK2399872A) is an effective and specific RIP3 kinase inhibitor. It binds RIP3 kinase domain with high affinity (IC50: 1.8 nM) and inhibits kinase activity (IC50: 1.3 nM).

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[1].

In compared with no treatment after ischemic injury in vivo, GSK872 can significantly reduce HIF-1α expression [3].

1346546-69-7

C19H17N3O2S2

383.48

GSK2399872A;GSK872;GSK'872

H2O:<1 mgml
DMSO:71 mg/mL (185.1 mM)
Ethanol:38 mg/mL (99.1 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years