cGAS inhibitor 3 is a potent, selective and covalent inhibitor of cyclic GMP-AMP synthase (cGAS) with cellular IC50 of 0.51 uM.
cGAS inhibitor 3 directly and covalently binds to Cys419 of cGAS.
cGAS inhibitor 3 displayed high potency and selectivity at the cellular level.
cGAS inhibitor 3 demonstrated promising therapeutic efficacy in a dextran sulfate sodium (DSS)-induced mouse colitis model.
cGAS inhibitor 3 exhibited better inhibitory activity and pathway selectivity than RU.521, which is a selective cGAS inhibitor with anti-inflammatory effects in vitro and in vivo.
