GNA002 ( GNA-002 )

Catalog No. M11601 CAS No. 1385035-79-9

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Datasheet

HNMR

HPLC

MSDS

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Product Name

GNA002
Note

Research use only, not for human use.
Brief Description

GNA002 (GNA-002) is a gambogenic acid (GNA) derivative that specifically and covalently binds to Cys668 within the EZH2-SET domain.
Description

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.
Synonyms

GNA-002
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

HMTase
Research Area

Cancer
Indication

——

CAS Number

1385035-79-9
Formula Weight

701.90
Molecular Formula

C42H55NO8
Purity

>98% (HPLC)
Solubility

——
SMILES

CCOCCNC(=O)C(=CCC12C(=O)C3CC(C14C(=C3)C(=O)C5=C(C(=C(C(=C5O4)CC=C(C)C)O)CC=C(C)CCC=C(C)C)O)C(O2)(C)C)C
Chemical Name

(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

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

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