An EZH2 inhibitor
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JQEZ5

Item No. 27457

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal 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
CAS Number
1913252-04-6
Molecular Formula
C30H38N8O2
Formula Weight
542.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Chloroform: 30 mg/ml
λmax
233, 283, 313, 364 nm
SMILES
CN1CCN(C2=NC=C(C3=CC(C(NCC4=C(CCC)C=C(C)NC4=O)=O)=C(C=NN5C(C)C)C5=N3)C=C2)CC1
InChi Code
InChI=1S/C30H38N8O2/c1-6-7-21-14-20(4)34-30(40)24(21)17-32-29(39)23-15-26(35-28-25(23)18-33-38(28)19(2)3)22-8-9-27(31-16-22)37-12-10-36(5)11-13-37/h8-9,14-16,18-19H,6-7,10-13,17H2,1-5H3,(H,32,39)(H,34,40)
InChi Key
LQTWDAYNGMMHLV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    25 mg

    $505

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    50 mg

    $894

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    Product Description

    JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2).1,2 It inhibits colony formation of primary human CD34+ chronic myelogenous leukemia (CML) stem/progenitor cells but not non-cancerous human CD34+ hematopoietic stem/progenitor cells when used at concentrations ranging from 0.5 to 5 µM.2 It also reduces global levels of trimethylated histone 3 lysine 27 (H3K27Me3), a mark that is regulated by PRC2, in K562 cells. JQEZ5 (75 mg/kg per day) induces regression of tumors in an EZH2-driven transgenic mouse model of lung adenocarcinoma.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bradner, J.E., Qi, J., and Wong, K.K. EZH2 inhibitors and uses thereof. (2016).

    2. Xie, H., Peng, C., Huang, J., et al. Chronic myelogenous leukemia-initiating cells require polycomb group protein EZH2. Cancer Discov. 6(11), 1237-1247 (2016).