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Chemical Structure : 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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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.
| M.Wt | 480.92 | |
| Formula | C25H22ClFN4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Duncan E Shaw, et al. J Med Chem. 2023 Jun 22;66(12):8130-8139.
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