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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-E3 Ubiquitin Ligase-SMURF1 inhibitor 29
SMURF1 inhibitor 29

Chemical Structure : SMURF1 inhibitor 29

CAS No.: 1824647-09-7

SMURF1 inhibitor 29

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 480.92
分子式 C25H22ClFN4O3
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

O=C(C1=NOC(C2=CC=C(C3CC3)C=C2Cl)=C1C)NC4=C(C)N(C)N(C5=CC=CC=C5F)C4=O

参考文献

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

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