GENERAL CATALOGUE
GNA002
HY-101508 · 1 mg
MedChemExpress · Cat: HY-101508
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Catalog No: HY-101508
CAS No: 1385035-79-9
Category: Epigenetics
Pack Size: 1 mg
Brand: MedChemExpress
Description
GNA002 is a highly potent, specific and covalent EZH2 Enhancer of zeste homolog 2 inhibitor with an IC50 of 1.1 ?M. 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.
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