JQEZ5

Name: JQEZ5
Brand: Tocris Bioscience
SKU: 6153

Tocris Bioscience, part of Bio-Techne | Catalog # 6153

COA / SDS

Potent and selective SAM-competitive EZH2 inhibitor

Key Product Details

Description:	Potent and selective SAM-competitive EZH2 inhibitor
Chemical Name:	N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-1H-pyrazolo[3,4-b]pyridine-4-carboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	542.69

View Full Technical Details for JQEZ5

Technical Data
Citations

Biological Activity for JQEZ5

JQEZ5 is a potent and selective SAM-competitive EZH2 lysine methyltransferase inhibitor (IC₅₀ = 11 nM). Selectively binds EZH2 over a panel of 22 methyltransferases. Reduces global level of the PRC2-associated mark H3K27me3 in K562 cells. Suppresses cell growth in CML cells. Inhibits colony formation of primary human CD34⁺ CML stem/ progenitor cells. Antitumor effects in vivo.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Compound Libraries for JQEZ5

JQEZ5 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for JQEZ5

M. Wt	542.69
Formula	C₃₀H₃₈N₈O₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1913252-04-6
PubChem ID	121322599
InChi Key	LQTWDAYNGMMHLV-UHFFFAOYSA-N
Smiles	CN(CC1)CCN1C2=CC=C(C3=NC(N(C(C)C)N=C4)=C4C(C(NCC5=C(CCC)C=C(C)NC5=O)=O)=C3)C=N2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for JQEZ5

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	10.85	20

Preparing Stock Solutions for JQEZ5

The following data is based on the product molecular weight 542.69.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	9.21 mL	46.07 mL	92.13 mL
1 mM	1.84 mL	9.21 mL	18.43 mL
2 mM	0.92 mL	4.61 mL	9.21 mL
10 mM	0.18 mL	0.92 mL	1.84 mL

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References for JQEZ5

References are publications that support the biological activity of the product.

Frankel Developing EZH2-targeted therapy for lung cancer. Cancer Discov. 2016 PMID: 27587466
Zhang Oncogenic deregulation of EZH2 as an opportunity for targeted therapy in lung cancer. Cancer Discov. 2016 PMID: 27312177
Xie Chronic myelogenous leukemia- initiating cells require polycomb group protein EZH2. Send to 2016 PMID: 27630126