cGAS inhibitor 3

Chemical Structure : cGAS inhibitor 3

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货号: PC-49403Not For Human Use, Lab Use Only.

cGAS inhibitor 3 is a potent, selective and covalent inhibitor of cyclic GMP-AMP synthase (cGAS) with cellular IC50 of 0.51 uM.

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生物&药学活性

cGAS inhibitor 3 is a potent, selective and covalent inhibitor of cyclic GMP-AMP synthase (cGAS) with cellular IC50 of 0.51 uM.
cGAS inhibitor 3 directly and covalently binds to Cys419 of cGAS.
cGAS inhibitor 3 displayed high potency and selectivity at the cellular level.
cGAS inhibitor 3 demonstrated promising therapeutic efficacy in a dextran sulfate sodium (DSS)-induced mouse colitis model.
cGAS inhibitor 3 exhibited better inhibitory activity and pathway selectivity than RU.521, which is a selective cGAS inhibitor with anti-inflammatory effects in vitro and in vivo.

物理化学性质&存储条件

分子量	250.301
分子式	C16H14N2O
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	1-(1-phenyl-3,4-dihydro-1H-pyrrolo[1,2-a]pyrazin-2-yl)prop-2-yn-1-one

参考文献

1. Jia Song, et al. Acta Pharmacol Sin. 2022 Oct 13. doi: 10.1038/s41401-022-01002-5.

cGAS inhibitor 3

生物&药学活性

物理化学性质&存储条件

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cGAS inhibitor 3

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物理化学性质&存储条件

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