Description
JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitive inhibition of polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects.
Product information
CAS Number: 1913252-04-6
Molecular Weight: 542.68
Formula: C30H38N8O2
Chemical Name: N-[(6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl]-6-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide
Smiles: CN1CCN(CC1)C1=CC=C(C=N1)C1=CC(=C2C=NN(C(C)C)C2=N1)C(=O)NCC1=C(CCC)C=C(C)NC1=O
InChiKey: LQTWDAYNGMMHLV-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 25 mg/mL (46.07 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
JQEZ5 inhibits enzymatic functionality of PRC2 with a biochemical IC50 of 80nM. JQEZ5 exhibits S-adenosyl methionine (SAM)-competitive inhibition of PRC2. H661 cells treated with increasing concentrations of JQEZ5 demonstrate acutely reduced levels of H3K27me3 without affecting H3K27 mono- or di-methylation. JQEZ5 suppresses the proliferation of EZH2-overexpressing H661 and H522 cells after treatment for 4 days without affecting the proliferation of cell lines that were deemed insensitive to EZH2 knockdown.
In Vivo:
JQEZ5 (75 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment exhibits rapid and pronounced tumor regression over the three week treatment course. And H3K27me3 levels are largely reduced with treatment further confirming the on-target effect of JQEZ5 in mice.
Products are for research use only. Not for human use.
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