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抑制剂描述:

产品名称:H-151

产品别名:见爱必信官网

英文别名:H-151

靶点:STING

CAS:941987-60-6

纯度:98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:H-151 is a highly potent, selective and covalent antagonist of STING, reduces TBK1 phosphorylation and suppresses human STING palmitoylation.

溶解性:DMSO : 125 mg/mL (447.48 mM; Need ultrasonic)

体外研究:

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.

体内研究: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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