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SMURF1 inhibitor 38

Chemical Structure : SMURF1 inhibitor 38

CAS No.: 1824708-03-3

SMURF1 inhibitor 38

Catalog No.: PC-20904Not For Human Use, Lab Use Only.

SMURF1 inhibitor 38 is a potent, specific E3 ubiquitin protein ligase 1 (SMURF1) inhibitor with biochemical IC50 of 92 nM, displays no activity against SMURF2.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SMURF1 inhibitor 38 is a potent, specific E3 ubiquitin protein ligase 1 (SMURF1) inhibitor with biochemical IC50 of 92 nM, displays no activity against SMURF2.
SMURF1 inhibitor 38 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 38 shows a clean safety pharmacology profile against a standard panel of ion channels and GPCRs.
SMURF1 inhibitor 38 (10 mg/kg) exhibits in vivo efficacy in the hypoxia/Sugen rat model of pulmonary hypertension.

Physicochemical Properties

M.Wt 468.99
Formula C24H29ClN6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C(NC1=C(C)N(C)N(C2CCCCC2)C1=O)C3=C(C)N(C4=C(Cl)C=C(C5CC5)C=C4)N=N3

References

1. Duncan E Shaw, et al. J Med Chem. 2023 Jun 22;66(12):8130-8139.

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