Chemical Structure : GNA002
Catalog No.: PC-35431Not For Human Use, Lab Use Only.
GNA002 (GNA-002) is a gambogenic acid (GNA) derivative that specifically and covalently binds to Cys668 within the EZH2-SET domain, trigges EZH2 degradation (IC50=1.1 uM) through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination.
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GNA002 (GNA-002) is a gambogenic acid (GNA) derivative that specifically and covalently binds to Cys668 within the EZH2-SET domain, trigges EZH2 degradation (IC50=1.1 uM) through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination.
GNA002 is a relatively more potent EZH2 interacting agent than GNA, significantly suppresses H3K27Me3 and effectively reactivated PRC2-silenced tumor suppressor genes.
M.Wt | 701.901 | |
Formula | C42H55NO8 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
1. Wang X, et al. EMBO J. 2017 May 2;36(9):1243-1260.
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