Smurf1 inhibitor 1

Chemical Structure : Smurf1 inhibitor 1

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货号: PC-21307Not For Human Use, Lab Use Only.

Smurf1 inhibitor 1 is a potent, selective Smurf1 E3 ligase inhibitor with IC50 of 230 nM in in UbFluor assays, inhibits the catalytic HECT domain of Smurf1.

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生物&药学活性

Smurf1 inhibitor 1 is a potent, selective Smurf1 E3 ligase inhibitor with IC50 of 230 nM in in UbFluor assays, inhibits the catalytic HECT domain of Smurf1.
Smurf1 inhibitor 1 inhibit E2-Ub/Smurf1 transthiolation and Ub propargyl labeling of Smurf1.
Smurf1 inhibitor 1 also blocks the covalent labeling of Smurf1 with the UbPA suggesting that it inhibits the function of the Cterminal FAVE peptide and may destabilize the L-conformation of Smurf1 HECT domain, or block the catalytic cysteine.
Smurf1 inhibitor 1 does not inhibits closely related Smurf2 ligase and other E3 ligases WWP1, Nedd4-1, and NleL.

物理化学性质&存储条件

分子量	522.54
分子式	C24H25F3N4O4S
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	N-(2-cyclohexyl-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazol-4-yl)-8-(trifluoromethoxy)-4,5-dihydrobenzo[6,7]thiepino[4,5-d]isoxazole-3-carboxamide

参考文献

1. Patrick Chuong, et al. bioRxiv. 2023 Oct 14:2023.10.14.562361.