GNA002 |
| Catalog No.GC36168 |
GNA002는 IC50이 1.1μM인 매우 강력하고 특이적이고 공유적인 EZH2(제스테 동족체 2의 증강 인자) 억제제입니다. GNA002는 EZH2-SET 도메인 내에서 Cys668에 특이적이고 공유적으로 결합하여 Hsp70-상호작용 단백질(CHIP) 매개 유비퀴틴화의 COOH 말단을 통해 EZH2 분해를 유발할 수 있습니다. GNA002는 EZH2 매개 H3K27 트리메틸화를 효율적으로 감소시키고 폴리콤 억제 복합체 2(PRC2) 침묵 종양 억제 유전자를 재활성화합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1385035-79-9
Sample solution is provided at 25 µL, 10mM.
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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[1]. EZH2|1.1 μM (IC50)
GNA002 (10 μM; 72 hours) clearly inhibits the proliferation of numerous cancer cell lines with IC50s of 0.070 μM and 0.103 μM for MV4-11 and RS4-11[1]. GNA002 (2 μM; 24 hours) demonstrates an elevated capacity to induce cell death in human cancer cells[1]. GNA002 (0.1-4 μM; 48 hours) efficiently reduces EZH2-mediated H3K27 trimethylation in Cal-27 head and neck cancer cells[1]. Cell Proliferation Assay[1] Cell Line: Numerous cancer cell lines
GNA002 (oral administration; 100 mg/kg; daily) significantly decreases the volumes of Cal-27-derived tumors and reduces H3K27Me3 levels in tumor tissues. GNA002 also significantly suppresses the in vivo tumor growth derived from the xenografted A549 lung cancer cells, Daudi and Pfeiffer cells. GNA002 inhibits the aberrant oncogenic functions of EZH2, thus inhibiting tumor growth in vivo, at least in the xenograft experimental model[1]. Animal Model: Male BALB/C Nude mice aged 30-35 days and weighing 18-22 g, bearing Cal-27 xenograft tumors[1]
[1]. Wang X, et al. A covalently bound inhibitor triggers EZH2 degradation through CHIP-mediated ubiquitination. EMBO J. 2017 May, 36(9):1243-1260.
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