Chemical Structure : Smurf1 inhibitor 1
CAS No.:
1825311-67-8
Smurf1 inhibitor 1
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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522.54
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Formula
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C24H25F3N4O4S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Patrick Chuong, et al. bioRxiv. 2023 Oct 14:2023.10.14.562361.
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