| Name | GSK963 |
| Description | GSK963 (Racemate), a structurally distinct, potent and selective inhibitor of RIP1 kinase(IC50=29 nM). |
| Kinase Assay | GSK′963 was tested against 339 kinases using a P33-radiolabeled assay at Reaction Corp Biology. The compound was tested at a single dose in duplicate at 10?μM. Reactions were carried out at 10?μM ATP. Data are reported as % enzyme activity (relative to DMSO controls). |
| In vitro | The increased potency of GSK 963 relative to Nec-1 in vitro also translated into increased efficacy in the TNF+zVAD-induced model of sterile shock.?At a dose of 2 mg/kg, GSK 963 was able to completely inhibit temperature loss in response to TNF+zVAD, ?the phenotype of the recently described RIP1 kinase-dead knock-in mice.?The level of inhibition of temperature loss in this acute model at different doses of GSK 963 was in line with the predictions of efficacy based on modeling of the pharamacokinetic profile and in vitro potency of GSK 963. |
| In vivo | GSK 963 efficiently blocked necroptosis in both murine and human cells with IC50 values of 1 nM and 4 nM, respectively, whereas the inactive analog GSK 962 was at least 1000-fold less potent in these assays. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 40 mg/mL (173.68 mM), Sonication is recommended.
10% DMSO+90% Corn Oil : 2 mg/mL (8.68 mM), Sonication is recommended.
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| Keywords | RIPkinase | RIP1 | RIP kinase | Racemate | GSK-963 | GSK963 | GSK 963 |
| 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 | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Liver Cancer Compound Library |
United States
