| Name | GSK-872 |
| Description | GSK-872 (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). |
| 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (10.43 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 141 mg/mL (367.68 mM), Sonication is recommended.
Ethanol : 38 mg/mL (99.09 mM), Sonication is recommended.
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| Keywords | translocation | RIPkinase | RIPK | RIP3K | RIP kinase | Receptor-interacting protein kinases | neurological | Inhibitor | inhibit | HMGB1 | GSK-872 | GSK 872 | edema | deficits | cytoplasmic | brain |
| Inhibitors Related | PK68 | Necrostatin-1 | RIPK2-IN-5 | Oditrasertib | Apostatin-1 | LY-364947 | RIPK2-IN-3 | Necroptosis-IN-1 | ICCB-19 hydrochloride | Necrostatin-34 | RIPA-56 | GSK2983559 free acid |
| Related Compound Libraries | Highly Selective Inhibitor Library | Apoptosis Compound Library | NF-κB Signaling Compound Library | Bioactive Compound Library | Antidepressant Compound Library | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
