JQEZ5

JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2). 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. 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.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: Chloroform: 30 mg/ml. lambdamax: 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.