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GNA002 is a potent, selective, covalent EZH2 inhibitor with an IC50 of 1.1 μM against EZH2. GNA002 can specifically and covalently bind Cys668 in the EZH2-SET domain to induce EZH2 degradation through COOH terminal of ubiquitination mediated by Hsp70 interacting protein (CHIP). GNA002 effectively reduced EZH2-mediated H3K27 trimethylation and reactivated tumor suppressor genes silenced by Polycomb repressor complex 2 (PRC2).
| Molecular Weight | 701.9 |
| Formula | C42H55NO8 |
| CAS Number | 1385035-79-9 |
| Solubility (25°C) | DMSO ≥ 20 mg/mL |
| Storage | -20°C, dry, sealed |
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