Bioactivity | GSK8612 is a highly selective and potent Tank-binding Kinase-1 (TBK1) inhibitor, with a pIC50 of 6.8 for recombinant TBK1[1]. |
Invitro | GSK8612 inhibits toll-like receptor (TLR)3-induced IRF3 phosphorylation in Ramos cells and type I IFN secretion in primary human mononuclear cells. In THP1 cells, GSK8612 is able to inhibit secretion of IFNβ in response to dsDNA and cGAMP, the natural ligand for STING[1]. |
Name | GSK8612 |
CAS | 2361659-62-1 |
Formula | C17H17BrF3N7O2S |
Molar Mass | 520.33 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -20°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
Reference | [1]. Thomson DW, et al. Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor. ACS Med Chem Lett. 2019 Mar 11;10(5):780-785. |