Chemical Structure : SMURF1 inhibitor 29
CAS No.:
1824647-09-7
SMURF1 inhibitor 29
Catalog No.: PC-20919Not For Human Use, Lab Use Only.
SMURF1 inhibitor 29 is a potent, specific E3 ubiquitin protein ligase 1 (SMURF1) inhibitor with biochemical IC50 of 11 nM, displays no activity against SMURF2.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
SMURF1 inhibitor 29 is a potent, specific E3 ubiquitin protein ligase 1 (SMURF1) inhibitor with biochemical IC50 of 11 nM, displays no activity against SMURF2.
SMURF1 inhibitor 29 also is highly selective against an E3 ligase panel consisting of ubiquitin-protein ligase E3A (UBE3A/E6AP), WW domain-containing protein 1/NEDD4-like E3 ubiquitin-protein ligase (WWP1), WW domain-containing protein 2 (Wwp2), neural precursor cell expressed developmentally downregulated protein 4 (Nedd4), Itch.
SMURF1 inhibitor 29 shows a clean safety pharmacology profile against a standard panel of ion channels and GPCRs.
SMURF1 inhibitor 29 (10 mg/kg) exhibits in vivo efficacy in the hypoxia/Sugen rat model of pulmonary hypertension.
Physicochemical Properties
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M.Wt
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480.92
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Formula
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C25H22ClFN4O3
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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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O=C(C1=NOC(C2=CC=C(C3CC3)C=C2Cl)=C1C)NC4=C(C)N(C)N(C5=CC=CC=C5F)C4=O
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References
1. Duncan E Shaw, et al. J Med Chem. 2023 Jun 22;66(12):8130-8139.
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