Synonym: 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
CAS Number: 2049868-46-2
Empirical Formula (Hill Notation): C14H18N2O
Molecular Weight: 230.31
Linear Formula: C14H18N2O
Product Type: Chemical
assay |
≥98% (HPLC) |
color |
white to beige |
form |
powder |
SMILES string |
O=C(C(C)(C)C)N1[C@H](C2=CC=CC=C2)CC=N1 |
solubility |
DMSO: 2 mg/mL, clear |
storage temp. |
2-8°C |
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 μM ATP; IC50 >10 μM against RIPK2/3/5 and 335 other kinases) that protects against TNFα/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 μM). GSK′963 prevents lethal hypothermia by acute sterile shock (2 mg/kg i.p. 15 min prior to TNFα/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.). |
WGK Germany |
WGK 3 |
Flash Point(F) |
Not applicable |
Flash Point(C) |
Not applicable |
Purity |
≥98% (HPLC) |
Storage Temp. |
2-8°C |
UNSPSC |
12352200 |