EPZ-6438

• CAT Number: I001546
• CAS Number: 1403254-99-8
• Molecular Formula: C₃₄H₄₄N₄O₄
• Molecular Weight: 572.74
• Purity: ≥95%
• Target: Histone Methyltransferase
• Solubility: DMSO: ≤ 6.2 mg/mL
• Storage: Desiccate at -20°C
• IC50: 2.5±0.5 nM (PRC2-containing wild-type EZH2) [1]
• InChI: InChI=1S/C34H44N4O4/c1-5-38(29-10-14-41-15-11-29)32-20-28(27-8-6-26(7-9-27)22-37-12-16-42-17-13-37)19-30(25(32)4)33(39)35-21-31-23(2)18-24(3)36-34(31)40/h6-9,18-20,29H,5,10-17,21-22H2,1-4H3,(H,35,39)(H,36,40)
• InChIKey: NSQSAUGJQHDYNO-UHFFFAOYSA-N
• SMILES: CCN(C1CCOCC1)C2=CC(C3=CC=C(CN4CCOCC4)C=C3)=CC(C(NCC5=C(C)C=C(C)NC5=O)=O)=C2C

EPZ-6438 (CAT: I001546) is a small-molecule inhibitor that specifically targets the enzymatic activity of enhancer of zest homolog 2 (EZH2). EZH2 is a histone methyltransferase enzyme involved in the epigenetic regulation of gene expression. By inhibiting the enzymatic activity of EZH2, EPZ-6438 disrupts the methylation of histone proteins, leading to alterations in gene expression patterns. EPZ-6438 is known for its potent and selective inhibition of EZH2, making it a valuable tool in studying the function and therapeutic potential of EZH2 in various diseases, including cancer.

Reference

1:Initial testing (stage 1) of tazemetostat (EPZ-6438), a novel EZH2 inhibitor, by the Pediatric Preclinical Testing Program. Kurmasheva RT, Sammons M, Favours E, Wu J, Kurmashev D, Cosmopoulos K, Keilhack H, Klaus CR, Houghton PJ, Smith MA.Pediatr Blood Cancer. 2017 Mar;64(3). doi: 10.1002/pbc.26218. Epub 2016 Aug 24. PMID: 27555605 2:No Significant Cytotoxic Effect of the EZH2 Inhibitor Tazemetostat (EPZ-6438) on Pediatric Glioma Cells with Wildtype Histone 3 or Mutated Histone 3.3. Wiese M, Schill F, Sturm D, Pfister S, Hulleman E, Johnsen SA, Kramm CM.Klin Padiatr. 2016 Apr;228(3):113-7. doi: 10.1055/s-0042-105292. Epub 2016 May 2. PMID: 27135271 3:Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma. Knutson SK, Kawano S, Minoshima Y, Warholic NM, Huang KC, Xiao Y, Kadowaki T, Uesugi M, Kuznetsov G, Kumar N, Wigle TJ, Klaus CR, Allain CJ, Raimondi A, Waters NJ, Smith JJ, Porter-Scott M, Chesworth R, Moyer MP, Copeland RA, Richon VM, Uenaka T, Pollock RM, Kuntz KW, Yokoi A, Keilhack H.Mol Cancer Ther. 2014 Apr;13(4):842-54. doi: 10.1158/1535-7163.MCT-13-0773. Epub 2014 Feb 21. PMID: 24563539 Free Article