BIIB129

BIIB129 is a covalent inhibitor of Bruton's tyrosine kinase (BTK). It is selective for BTK over a panel of 403 additional kinases at 1 µM. BIIB129 inhibits CD69 activation in isolated human whole blood (IC50 = 7.9 nM). In vivo, BIIB129 inhibits anti-myelin oligodendrocyte glycoprotein (MOG) antibody-induced microglia activation in mice (ED50 = 1.5 mg/kg). SMILES C[C@](C[C@H]1N(C)C(C=C)=O)(C1)OC2=NC(C(C=N3)=CN3C)=CN4C2=CC=N4 InChi Code InChI=1S/C19H22N6O2/c1-5-17(26)24(4)14-8-19(2,9-14)27-18-16-6-7-20-25(16)12-15(22-18)13-10-21-23(3)11-13/h5-7,10-12,14H,1,8-9H2,2-4H3/t14-,19+ InChi Key WBFSPPPOPIJCLF-DHFPXDALSA-N