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GNA002
$950 – $1,520
Products Details
Product Description
– 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].
Web ID
– HY-101508
Storage Temperature
– -20°C (Powder, stored under nitrogen)
Shipping
– Blue Ice
Applications
– Cancer-programmed cell death
Molecular Formula
– C42H55NO8
References
– [1]Wang X, et al. A covalently bound inhibitor triggers EZH2 degradation through CHIP-mediated ubiquitination. EMBO J. 2017 May, 36(9):1243-1260.
CAS Number
– 1385035-79-9
Molecular Weight
– 701.89
Compound Purity
– 98.05
SMILES
– O=C(NCCOCC)/C(C)=CC[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
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– DMSO : 25 mg/mL (ultrasonic)
Target
– Histone Methyltransferase
Isoform
– EZH2
Pathway
– Epigenetics
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
