| Bioactivity | 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[1]. | |||||||||
| Target | STING | |||||||||
| Invitro | H-151 (0.02-2 μM) reduces IFNβ luciferase reporter measurements of HEK293T cells[1].H-151 (0.5 μM; 2 h) inhibits the phosphorylation of TBK1 in THP-1 cells[1].H-151 (1 μM; 3 h) suppresses hsSTING palmitoylation[1]. | |||||||||
| In Vivo | H-151 (750 nmol per mouse; a single i.p.) markedly reduces systemic cytokine responses in CMA-treated mice[1].H-151 (750 nmol per mouse; i.p. daily for 7 d) exhibits notable efficacy in Trex1−/− mice that expressed a bioluminescent IFNβ reporter[1].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[1]. | |||||||||
| Name | H-151 | |||||||||
| CAS | 941987-60-6 | |||||||||
| Formula | C17H17N3O | |||||||||
| Molar Mass | 279.34 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Haag SM, et al. Targeting STING with covalent small-molecule inhibitors. Nature. 2018 Jul;559(7713):269-273. |