GSK8612

GSK8612 is an inhibitor of TANK-binding kinase 1 (TBK1, IC50 = 158 nM). It is selective for TBK1 over a panel of 285 kinases. GSK8612 inhibits IFN-alpha release in isolated human peripheral blood mononuclear cells (PBMCs) stimulated with polyinosinic-polycytidylic acid (poly(I:C), IC50 = 794 nM). It also inhibits IFN-beta 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).Formal Name: 4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]amino]-4-pyrimidinyl]amino]methyl]-benzenesulfonamide. CAS Number: 2361659-62-1. Molecular Formula: C17H17BrF3N7O2S. Formula Weight: 520.3. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/mL, DMSO: 5 mg/mL, PBS (pH 7.2): 0.3 mg/mL. lambdamax: 228 nm. SMILES: NS(C1=CC=C(CNC2=C(Br)C=NC(NC3=CN(CC(F)(F)F)N=C3C)=N2)C=C1)(=O)=O. InChi Code: InChI=1S/C17H17BrF3N7O2S/c1-10-14(8-28(27-10)9-17(19,20)21)25-16-24-7-13(18)15(26-16)23-6-11-2-4-12(5-3-11)31(22,29)30/h2-5,7-8H,6,9H2,1H3,(H2,22,29,30)(H2,23,24,25,26). InChi Key: FFPHMUIGESPOTK-UHFFFAOYSA-N.