2361659-62-1

GSK8612 (2361659-62-1) is a highly selective and potent (avg. pIC50 = 6.8 versus recombinant TBK1) inhibitor of Tank-binding Kinase-1 (TBK1) with higher affinity for unactivated TBK1.? It inhibited phosphorylation of IRF3 (pIC50 = 6.0), inhibited the release of IFNa from human PBMC’s (pIC50 = 6.1), and inhibited IFNb secretion from THP-1 cells (pIC50 = 5.8 dsDNA virus, 6.3 cGAMP stilmulated cells).

GSK 8612 is a highly selective TBK1 Inhibitor involved in regulating signaling pathways in immune responses.

Thomson et al. (2019), Discovery of a GSK8612, a Highly Selective and Potent TBK1 Inhibitor; ACS Med. Chem. Lett., 10 780