H-151

H-151CAS号: 941987-60-6分子式: C17H17N3O分子量: 279.34描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
H-151 is a highly potent, selective and covalent antagonist of STING, reduces TBK1 phosphorylation and suppresses human STING palmitoylation.
纯度
98%
储存/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.
基本信息
别名
H 151
外观
White to off-white solid
可溶性/溶解性
DMSO : 125 mg/mL (447.48 mM; Need ultrasonic)
生物活性
靶点
STING
In vitro(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.
In vivo(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.

分子结构图

H-151