ML-364

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. 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.Formal Name: 2-[[(4-methylphenyl)sulfonyl]amino]-N-(4-phenyl-2-thiazolyl)-4-(trifluoromethyl)-benzamide. CAS Number: 1991986-30-1. Molecular Formula: C24H18F3N3O3S2. Formula Weight: 517.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml, Ethanol: 20 mg/ml. lambdamax: 232, 329 nm. SMILES: [H]N(C(C1=C(N(S(C2=CC=C(C)C=C2)(=O)=O)[H])C=C(C(F)(F)F)C=C1)=O)C3=NC(C4=CC=CC=C4)=CS3. InChi Code: InChI=1S/C24H18F3N3O3S2/c1-15-7-10-18(11-8-15)35(32,33)30-20-13-17(24(25,26)27)9-12-19(20)22(31)29-23-28-21(14-34-23)16-5-3-2-4-6-16/h2-14,30H,1H3,(H,28,29,31). InChi Key: QZUGMNXETPARLI-UHFFFAOYSA-N.