Formulation: A solid
Formal Name: 4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]amino]-4-pyrimidinyl]amino]methyl]-benzenesulfonamide
Purity: ≥95%
Formula Markup: C17H17BrF3N7O2S
Formula Weight: 520,3
Shelf life (days): 1460
CAS Number: 2361659-62-1
Notes: GSK8612 is an inhibitor of TANK-binding kinase 1 (TBK1; IC50 = 158 nM).{50249} It is selective for TBK1 over a panel of 285 kinases. GSK8612 inhibits IFN-α release in isolated human peripheral blood mononuclear cells (PBMCs) stimulated with polyinosinic-polycytidylic acid (poly(I:C); IC50 = 794 nM). It also inhibits IFN-β secretion in THP-1 cells stimulated with dsDNA-containing baculovirus or cGAMP (IC50s = 1,258 and 501 nM, respectively). GSK8612 (5 mg/kg) reduces tumor volume and increases the number of tumor-infiltrating CD8+ T cells in immunocompetent, but not immunodeficient, mice in a model of carbon tetrachloride-induced hepatocellular carcinoma (HCC).{62746}
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