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JQEZ5

Chemical Structure : JQEZ5

CAS No.: 1913252-04-6

JQEZ5 (JQ5;EZ005;JQEZ-5)

Catalog No.: PC-60263Not For Human Use, Lab Use Only.

JQEZ5 (JQ5, EZ005) is a novel potent, selective, SAM-competitive EZH2 inhibitor with IC50 of 80 nM (inhibition of enzymatic function of PRC2).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

JQEZ5 (JQ5, EZ005) is a novel potent, selective, SAM-competitive EZH2 inhibitor with IC50 of 80 nM (inhibition of enzymatic function of PRC2).
JQEZ5 demonstrates acutely reduced level of H3K27me3 without affecting mono- and di-methylation, suppresses the proliferation of EZH2-overexpression H661 and H522 cell lines, more effectively than GSK-126 and GSK-343.
JQEZ5 promotes the regression of EZH2-driven tumors in vivo.

Physicochemical Properties

M.Wt 542.688
Formula C30H38N8O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-propan-2-ylpyrazolo[3,4-b]pyridine-4-carboxamide

References

1. Zhang H, et al. Cancer Discov. 2016 Sep;6(9):1006-21.

2. Frankel AE, et al. Cancer Discov. 2016 Sep;6(9):949-52.

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