GNA002

Overview

GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC 50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes.

Application

Products | Products > Signaling Pathways > Epigenetics | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > Histone Methyltransferase

Product Information

• Catalog No.: HY-101508
• CAS No.: 1385035-79-9
• Molecular Formula: C42H55NO8
• Molecular Weight: 701.89
• Purity: 98.02%
• Storage: -20°C, stored under nitrogen * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
• Solubility: ≥ 1.25 mg/mL (1.78 mM); Clear solution
• Availability: In-stock

Source

Original product source