Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK872 HCl(1346546-69-7 free base) (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).
説明 | GSK872 HCl(1346546-69-7 free base) (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). |
ターゲット&IC50 | RIP3K:1.8 nM |
In vitro | 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 vivo | In compared with no treatment after ischemic injury in vivo, GSK872 can significantly reduce HIF-1α expression [3]. |
別名 | GSK2399872A |
分子量 | 419.94 |
分子式 | C19H18ClN3O2S2 |
CAS No. | 2703752-81-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (260.76 mM)
You can also refer to dose conversion for different animals. 詳細
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