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H-151

CAS No. : 941987-60-6

產(chǎn)品活性：H-151 is a potent, selective and covalent antagonist of STING that has noteworthy inhibitory activity both in cells and in vivo. H-151 reduces TBK1 phosphorylation and suppresses STING palmitoylation. H-151 can be used for the research of autoinflammatory disease.

研究領(lǐng)域：Immunology/Inflammation

作用靶點(diǎn)：STING

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.

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