An inhibitor of USP2 (IC50 = 1.1 µM); inhibits the closely related USP8 (IC50 = 0.95 µM); no activity at multiple proteases or 102 kinases

ML-364 – 1 mg

Brand:
Cayman
CAS:
1991986-30-1
Storage:
-20
UN-No:
Non-Hazardous - /

ML-364 is a reversible inhibitor of ubiquitin-specific protease 2 (USP2), a deubiquitinase, that has an IC50 value of 1.1 µM in a fluorescence-based assay using di-ubiquitin substrates.{39305} It inhibits USP8, which is closely related to USP2, with an IC50 value of 0.95 µM in the same assay. It has no activity at the proteases caspase-6, caspase-7, MMP-1, MMP-9, and USP15 or at 102 kinases in a panel including cell cycle regulators. ML-364 increases cyclin D1 degradation (IC50 = 0.97 µM) in HCT116 colorectal carcinoma cells. It induces arrest of the cell cycle at the G1 phase in Mino mantle cell lymphoma and HCT116 cells and inhibits proliferation of HCT116 cells (IC50 = 3.6 µM). It also decreases homologous recombination-mediated DNA repair in DR-GFP U2OS cells.  

 

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Description

An inhibitor of USP2 (IC50 = 1.1 µM); inhibits the closely related USP8 (IC50 = 0.95 µM); no activity at multiple proteases or 102 kinases, including cell cycle regulators; increases cyclin D1 degradation in HCT116 cells; induces cell cycle arrest at the G1 phase in Mino and HCT116 cells; inhibits proliferation of HCT116 cells (IC50 = 3.6 µM); decreases homologous recombination-mediated DNA repair in DR-GFP U2OS cells,

Formal name: 2-[[(4-methylphenyl)sulfonyl]amino]-N-(4-phenyl-2-thiazolyl)-4-(trifluoromethyl)-benzamide

Synonyms: 

Molecular weight: 517.5

CAS: 1991986-30-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Ubiquitin Ligase System||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|DNA Damage and Repair||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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