STING agonist diABZI compound 3 (diABZI-3) is an amidobenzimidazole (ABZI)-based compound that functions as a potent, specific, non-nucleotide STING agonist, induces dose-dependent activation of STING and secretion of IFN-β with EC50 of 130 nM in human PBMCs.
STING agonist diABZI compound 3 (diABZI-3) is an amidobenzimidazole (ABZI)-based compound that functions as a potent, specific, non-nucleotide STING agonist, induces dose-dependent activation of STING and secretion of IFN-β with EC50 of 130 nM in human PBMCs.
STING agonist diABZI compound 3 is more than 400-fold more potent than cGAMP, also demonstrates high selectivity against >350 kinases.
STING agonist diABZI compound 3 activates secretion of IFNβ, IL-6, TNF, and KC/GROα (also known as CXCL1) in wild-type but not Sting−/− mice, induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo via subcutaneous injection.
STING agonist diABZI compound 3 exhibits durable anti-tumour effect and causes complete tumour regression in syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice.
物理化学性质&存储条件
分子量
959.328
分子式
C42H54Cl3N13O7
外观性状
Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
(E)-1-(4-(5-Carbamoyl-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-(3-morpholinopropoxy)-1Hbenzo[d]imidazol-1-yl)but-2-en-1-yl)-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-methoxy-1Hbenzo[d]imidazole-5-carboxamide tris hydrochloride
参考文献
1. Ramanjulu JM, et al. Nature. 2018 Nov 7. doi: 10.1038/s41586-018-0705-y.
