H-151

H-151 is a highly potent selective and covalent antagonist of STING reduces TBK1 phosphorylation and suppresses human STING palmitoylation. (In Vitro) :H-151 (0.02-2 μM) reduces IFNβ luciferase reporter measurements of HEK293T cells.H-151 (0.5 μM; 2 h) inhibits the phosphorylation of TBK1 in THP-1 cells.H-151 (1 μM; 3 h) suppresses hsSTING palmitoylation. (In Vivo) :H-151 (750 nmol per mouse; a single i.p.) markedly reduces systemic cytokine responses in CMA-treated mice.H-151 (750 nmol per mouse; i.p. daily for 7 d) exhibits notable efficacy in Trex1 / mice that expressed a bioluminescent IFNβ reporter.H-151 (750 nmol per mouse; i.p.) reaches effective systemic levels, displays a short half-life in the serum and forms an adduct to mmSTING in wild-type mice.