2138300-40-8
2138300-40-8 结构式
基本信息
1H-Benzimidazole-5-carboxamide, 1,1'-(1,4-butanediyl)bis[2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-
物理化学性质
常见问题列表
IC50: 20 nM (STING agonist-4)
STING agonist-4 (Compound 2) (0.3-30 μM; 2 hours) causes phosphorylation of IRF3 and STING that is inhibited by the TBK1 inhibitor BX795 and induces dose-dependent secretion of IFN-β with an EC 50 of 3.1 μM. STING agonist-4 (Compound 2) (0.001 nM-1 μM) inhibits binding of full-length STING to the solid support with an apparent dissociation constant (K d ) of approximately 1.6 nM. STING agonist-4 (Compound 2) (0-100 μM) is 18-fold more potent than cGAMP (an endogenous STING ligand), with an EC 50 of 53.9 μM. STING agonist-4 (Compound 2) (3 μM; 4 hours) promotes production of interferon γ-induced protein 10 (IP-10), IL-6 and TNF-α by a mechanism that is dependent on STING-mediated activation of TBK1.
Cell Viability Assay
| Cell Line: | Human peripheral blood mononuclear cells (PBMCs) |
| Concentration: | 0.3 μM, 1 μM, 3 μM, 10 μM and 30 μM |
| Incubation Time: | 2 hours |
| Result: | Caused phosphorylation of IRF3 and STING and induced secretion of IFN-β. |