GNA002

MedChem Express

GNA002 [1385035-79-9]

10

1385035-79-9

Research Use Only

98.02

C42H55NO8

701.89

GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC 50 of 1.1 microM. 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 [1] .

O=C(NCCOCC)/C(C)=C\C[C@@]1(C2=O)OC(C)(C)[C@]([C@]31OC4=C5C(O)=C(C/C=C(C)/CC/C=C(C)\C)C(O)=C4C/C=C(C)\C)([H])C[C@@]2([H])C=C3C5=O

-20°C

12352200