| Bioactivity | GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro[1]. | ||||||||||||
| Target | IC50: 29 nM (RIP1 in FP binding assay). | ||||||||||||
| Invitro | GSK963 is >10 000-fold selective for RIP1 over 339 other kinases, lacks measurable activity against IDO and has an inactive enantiomer, GSK962, which can be used to confirm on-target effects[1]. | ||||||||||||
| In Vivo | GSK963 (2 mg/kg) results in a complete protection from TNF+zVAD-induced temperature loss. GSK963 (0.2 mg/kg) also shows a significant response[1]. Animal Model: | ||||||||||||
| Name | GSK963 | ||||||||||||
| CAS | 2049868-46-2 | ||||||||||||
| Formula | C14H18N2O | ||||||||||||
| Molar Mass | 230.31 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Berger SB, et al. Characterization of GSK'963: a structurally distinct, potent and selective inhibitor of RIP1 kinase. Cell Death Discov. 2015 Jul 27;1:15009. |