STING inhibitor SI-43

Chemical Structure : STING inhibitor SI-43

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货号: PC-24633Not For Human Use, Lab Use Only.

STING inhibitor SI-43 is a potent small molecule inhibitor of stimulator of interferon genes (STING) with IC50 of 0.11 uM against cGAMP-induced STING activation in THP1-Blue ISG cells.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

STING inhibitor SI-43 is a potent small molecule inhibitor of stimulator of interferon genes (STING) with IC50 of 0.11 uM against cGAMP-induced STING activation in THP1-Blue ISG cells.
SI-43 effectively inhibited cGAMP-induced release of IFN-β and CXCL-10 and blocked STING pathway signaling.
SI-43 induced proteasome-independent degradation of the SAVI-associated mutants STING S154 and STIN GM155, while sparing STING R232 and mSTING.
SI-43 binds to two coupled pockets of a STING dimer in its open conformation.
SI-43also able to inhibit STING activation induced by diABZI.
SI-43 shows low nanomolar inhibitory activity in THP1 cells harboring STINGR232, the wild-type STING with 60% of frequency in the human population.
SI-43 exhibits potent inhibition against cGAMP-induced mouse STING (mSTING) activation in THP1 cells (IC50 = 0.02-0.03 uM).
SI-43 (0.05–0.5 μM) significantly reduced IFN-β and CXCL-10 secretion in THP1 cells and bone marrow-derived macrophages (BMDM) isolated from mice, which is >10-fold more potent than SN-011.
SI-43 dramatically decreased cGAMP-induced phosphorylation of both STING and IRF3 in THP1-Blue ISG cells.
SI-43 (20 mg/kg PO, or 10 mg/kg, SC) demonstrated in vivo efficacy in cGAMP-induced autoimmune disease mouse model.

物理化学性质&存储条件

分子量	790.86
分子式	C43H39FN4O8S
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	2-(4-(tert-Butyl)-3-fluorophenyl)-3-(5-(4-((4-hydroxy-3-(methylsulfonamido)phenyl)carbamoyl)phenyl)benzofuran-2-yl)-7-methoxy-1-oxo-1,2,3,4-tetrahydroisoquinoline-4-carboxamide

参考文献

1. Zhao HY, et al. J Med Chem. 2025 May 19. doi: 10.1021/acs.jmedchem.5c00123.