ML364

SKU: orb1225763

Description

A potent, selective, reversible deubiquitinase USP2 inhibitor with IC50 of 1.1 uM in biochemical assay; also inhibits USP8 (IC50=0.95 uM), shows no against caspase 6/7, MMP1, MMP9 and USP15 and a panel of 102 kinase; increases cellular cyclin D1 degradation and causes cell cycle arrest and shows antiproliferative in cancer cell lines; also decreases homologous recombination-mediated DNA repair.

Key Properties

• CAS Number: 1991986-30-1
• MW: 517.5432296
• Purity: >98% (HPLC)
• Formula: C₂₄H₁₈F₃N₃O₃S₂
• SMILES: O=C(NC1=NC(C2=CC=CC=C2)=CS1)C3=CC=C(C(F)(F)F)C=C3NS(=O)(C4=CC=C(C)C=C4)=O
• Target: DUB
• Solubility: DMSO: ≥ 33 mg/mL

Bioactivity

• In Vitro:
  ML364 (5-20 μM; 24-48 hours) inhibits LnCAP and MCF7 cells viability in a dose-dependent manner. ML364 (10 μM; 2-24 hours) reduces cyclin D1 protein levels in a time-, dose-, and proteasome-dependent manner in HCT116 cells and Mino cells. Cell Viability Assay Cell line: LnCAP, MCF7 cells. Concentration: 5, 10, 15, 20 μM. Incubation time: 24, 48 hours. Result: LnCAP and MCF7 cells showed a decrease in cell viability in a dose-dependent manner. Western blot analysis. Cell line: HCT116, Mino cells. Concentration: 2, 4, 8, 16, 24 hours. Incubation time: 10 μM. Result: Reduced cyclin D1 protein levels in a time-, dose-, and proteasome-dependent manner in HCT116 cells and Mino cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ML 364 | ML-364

Quick Database Links

Gene Symbol

DUB