GNA002 |CAS:1385035-79-9 Probechem Biochemicals

Chemical Structure : GNA002

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GNA002 (GNA-002)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	701.901
分子式	C42H55NO8
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(Z)-4-((1S,3aR,5S,12aS)-9-((E)-3,7-dimethylocta-2,6-dien-1-yl)-8,10-dihydroxy-2,2-dimethyl-11-(3-methylbut-2-en-1-yl)-4,7-dioxo-1,2,5,7-tetrahydro-1,5-methanofuro[2,3-d]xanthen-3a(4H)-yl)-N-(2-ethoxyethyl)-2-methylbut-2-enamide

参考文献

1. Wang X, et al. EMBO J. 2017 May 2;36(9):1243-1260.

GNA002 (GNA-002)

生物&药学活性

物理化学性质&存储条件

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GNA002 (GNA-002)

生物&药学活性

物理化学性质&存储条件

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