JQEZ-5 ( EZ-005;EZ005;JQEZ5 )

Catalog No. M12997 CAS No. 1913252-04-6

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Product Name

JQEZ-5
Note

Research use only, not for human use.
Brief Description

A novel potent, selective, SAM-competitive EZH2 inhibitor with IC50 of 80 nM (inhibition of enzymatic function of PRC2).
Description

A novel potent, selective, SAM-competitive EZH2 inhibitor with IC50 of 80 nM (inhibition of enzymatic function of PRC2); 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; promotes the regression of EZH2-driven tumors in vivo.
Synonyms

EZ-005;EZ005;JQEZ5
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

HMTase
Research Area

——
Indication

——

CAS Number

1913252-04-6
Formula Weight

542.69
Molecular Formula

C30H38N8O2
Purity

>98% (HPLC)
Solubility

DMSO : 25 mg/mL 46.07 mM;H2O : < 0.1 mg/mL
SMILES

CC(C)N1N=CC2=C(C=C(N=C12)C3=CC=C(N4CCN(CC4)C)N=C3)C(NCC5=C(CCC)C=C(C)NC5=O)=O
Chemical Name

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

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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