EPZ-6438

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    EPZ-6438 is a potent and bio-available inhibitor of EZH2, the catalytic subunit of polycomb repressive complex 2 (PRC2) catalyzing the methylation of lysine 27 of histone H3 (H3K27), that inhibits the activity of human PRC2-containing wild-type EZH2 with a value of inhibition constant Ki of 2.5 nM. EPZ-6438 competitively binds to the S-adenosylmethionine (SAM) binding site of EZH2 and also non-competitively binds to the binding sites of peptide or nucleosome substrate. EPZ-6438 selectively inhibits EZH2 with selectivity 35-fold greater than EZH1. Study results have suggested that EPZ-6438 exhibits dramatic and permanent anti-tumor activity in MRT models through synergistic effects of EPZ-6438-mediated EZH2 inhibition on several cancer pathways.
- Properties
  - Alternative Name
    
    E-7438; N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide
    
    CAS Number
    
    1403254-99-8
    
    Molecular Formula
    
    C34H44N4O4
    
    Molecular Weight
    
    572.74
    
    Appearance
    
    A solid
    
    Purity
    
    99.66%
    
    Solubility
    
    ≥28.64 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Desiccate at -20°C
    
    * For Research Use Only
- Reference
  - 1. Fumiya Moribe, Momoko Nishikori, et al. "Epigenetic suppression of SLFN11 in germinal center B-cells during B-cell development." PLoS One. 2021 Jan 29;16(1):e0237554. PMID:33513156
    2. Otsuka Y, Nishikori M, et al. "EZH2 inhibitors restore epigenetically silenced CD58 expression in B-cell lymphomas." Mol Immunol. 2020;119:35–45. PMID:31962268
    3. Anastassiia Vertii, Jianhong Ou, et al. "Two Contrasting Classes of Nucleolus-Associated Domains in Mouse Fibroblast Heterochromatin." bioRxiv. 2018 December 03.
    4. Jiang S, Zhou H, et al. "The Epstein-Barr Virus Regulome in Lymphoblastoid Cells." Cell Host Microbe. 2017 Oct 11;22(4):561-573.e4. PMID:29024646
    5. Arifuzzaman S, Das A, et al. "Selective inhibition of EZH2 by a small molecule inhibitor regulates microglial gene expression essential for inflammation." Biochem Pharmacol. 2017 Apr 19. pii: S0006-2952(17)30233-2. PMID:28431938
    6. Wang H, Tian L, et al. "Bone-in-culture array as a platform to model early-stage bone metastases and discover anti-metastasis therapies." Nat Commun. 2017 Apr 21;8:15045. PMID:28429794
    7. Xia B, Gerstin E, et al. "Transgenerational programming of longevity through E(z)-mediated histone H3K27 trimethylation in Drosophila." Aging (Albany NY). 2016 Nov 25;8(11):2988-3008. PMID:27889707

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Background

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