Synonyms: 1-[(5S)-4,5-Dihydro-5-phenyl-1H-pyrazol-1-yl]-2,2-dimethyl-1-propanone; 2,2-Dimethyl-1-(5(S)-phenyl-4,5-dihydro-pyrazol-1-yl)-propan-1-one; GSK 963; GSK' 963A; GSK'963A; GSK-963; GSK-963A; GSK963; GSK963A
Molecular Formula: C14H18N2O
Molecular Weight: 230.31
Linear Structural Formula: C14H18N2O
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: GSK'963 (GSK'963A) is a brain-penetrant, highly potent and selective ATP site-targeting receptor-interacting protein 1 kinase (RIP1; RIPK1) inhibitor (IC50 = 0.8-8 nM with 50 muM ATP; IC50 >10 muM against RIPK2/3/5 and 335 other kinases) that protects against TNFalpha/zVAD-induced necroptosis (EC50 = 1/4 nM in mouse L929/human U937 cultures) and blocks Y. pestis-induced death of murine fetal liver macrophages (1 muM). GSK'963 prevents lethal hypothermia by acute sterile shock (2 mg/kg i.p. 15 min prior to TNFalpha/zVAD i.v.) and protects against acute neuronal death upon autologous blood intracerebral hemorrhage induction in mice in vivo (25 mg/kg/3 hr i.p.).