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GNA002
CAS No. : 1385035-79-9
Biological Activity：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.
Research Area：Cancer
Targets：Histone Methyltransferase
Related Screening Libraries:Bioactive Compound Library Plus;
Related Small Molecules:EEDi-5285;EZH2-IN-2;BIX-01294;SGC707;(S)-HH2853;G9a-IN-1;UNC4976;MS1943;OTS186935 hydrochloride;MS8815;(R)-HH2853;EPZ020411;Furamidine dihydrochloride;EZH2-IN-12;UNC0642;MU1656;Chaetocin;UNC0646;UNC0224;MRK-740;SMYD2-IN-1;PRMT5-IN-21;Sinefungin;MM-401;SETDB1-TTD-IN-1;Dot1L-IN-2;PRMT5-IN-10;PRMT1-IN-1
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