2 Results for "

covalent EZH2 degrader

" in MedChemExpress (MCE) Product Catalog:
Products (2)

2 Results for "covalent EZH2 degrader" in MCE Product Catalog:

Cat. No.: HY-101508
CAS No.: 1385035-79-9
Purity:  98.02%
Research Areas:  

Cancer

GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 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 .
loading...
    loading...
Cat. No.: HY-156292
CAS No.: 3018914-66-1
Research Areas:  

Cancer

IHMT-EZH2-426 is an orally active and selective EZH2 degrader. IHMT-EZH2-426 forms a covalent bond with Cys663 of EZH2, inhibits its catalytic activity, and reduces the protein levels of EZH2 as well as the level of H3K27me3. IHMT-EZH2-426 acts as an antiproliferative agent against B-cell lymphoma and triple-negative breast cancer cells, and also exhibits anti-tumor related activity in Pfeiffer and MDA‑MB‑231 xenograft models. IHMT-EZH2-426 can be used in studies related to B-cell lymphoma and triple-negative breast cancer .
loading...
    loading...