Synonyms: 4-(((5-Bromo-2-((3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)amino)methyl)benzenesulfonamide; 4-((5-Bromo-2-(3-methyl-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-ylamino)pyrimidin-4-ylamino)methyl)benzenesulfonamide; GSK 8612; GSK-8612
Molecular Formula: C17H17BrF3N7O2S
Molecular Weight: 520.33
Linear Structural Formula: C17H17BrF3N7O2S
MDL Number: MFCD32062739
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: GSK8612 is a potent and highly selective tank-binding kinase-1 (TBK1) inhibitor (pIC50 = 6.8; pKd = 8.0 vs pKa = 6.2/STK17B, 6.0/IKKepsilon, 6.1/LRRK2, 6.0/FLT4, 5.8/ULK3, 5.7/BMP2K, 5.7/CSNK2A1, 5.6/CSNK2A2, 5.6/FLT4, 5.5/PIK3CD,<5.5 ore than 270 kinases). gsk8612 inhibits ifnbeta secretion induced by dsdna containing virus or sting ligand cgamp (ic50="1.25" & 0.5 mum, respectively; thp-1), as well as suppresses tlr3 ligand poly(i:c)-induced irf3 ser396 phosphorylation (ic50="1" mum; ramos) and ifnalpha release (ic50="0.79" mum; human pbmcs), a ifn positive feedback response steming from ifnbeta.<>