G150 is a potent, specific human cyclic GMP-AMP synthase (cGAS) small-molecule inhibitor with IC50 of 10.2 nM, shows no inhibition against m-cGAS.
G150 binds to apo h-cGASCD, localized within the ATP and GTP binding pocket.
G150 showed dose-dependent inhibitory activity in THP1 cells with IC50 of 1.96 uM, as determined by qRT-PCR for IFNB1 mRNA.
G150 shows no off-target effect against other nucleotidyl transferase enzymes.
G150 inhibits the SEAP NF-κB pathway reporter with IC50 of 0.9 uM.
