GSK343, histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor (ab218610)

Overview

  • Product name

    GSK343, histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor
  • Description

    Potent, selective, cell-permeable histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor
  • Alternative names

    • GSK 343
    • N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide
    • N-[(6-Methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-(propan-2-yl)-1H-indazole-4-carboxamide
  • Biological description

    Potent, selective, cell-permeable histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor.  Inhibits EZH2 enzymatic activity (IC50 = 4 nM). Displays 60 fold selectivity for EZH2 over EZH1, and 1000 fold or greater selectivity against other histone methyltransferases. Inhibits H3K27 methylation in HCC1806 cells (IC50 < 200 nM).

  • Purity

    > 99%
  • CAS Number

    1346704-33-3
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    1-Isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(2-(4-methylpiperazin-1-yl)pyridine-4-yl)-1H-indazole-4-carboxamide
  • Molecular weight

    541.69
  • Molecular formula

    C31H39N7O2
  • PubChem identifier

    71268957
  • Storage instructions

    Shipped at 4°C. Store at -20°C. Store under desiccating conditions.
  • Solubility overview

    Soluble in DMSO to 25 mM
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC(=NC=C4)N5CCN(CC5)C)C(C)C
  • Source

    Synthetic

References

This product has been referenced in:

  • Ihira K  et al. EZH2 inhibition suppresses endometrial cancer progression via miR-361/Twist axis. Oncotarget N/A:N/A (2017). Read more (PubMed: 28088786) »
  • Liu TP  et al. S-Adenosyl-L-methionine-competitive inhibitors of the histone methyltransferase EZH2 induce autophagy and enhance drug sensitivity in cancer cells. Anticancer Drugs 26:139-47 (2015). Read more (PubMed: 25203626) »
  • Amatangelo MD  et al. Three-dimensional culture sensitizes epithelial ovarian cancer cells to EZH2 methyltransferase inhibition. Cell Cycle 12:2113-9 (2013). Read more (PubMed: 23759589) »
  • Verma SK  et al. Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett 3:1091-6 (2012). Read more (PubMed: 24900432) »

Customer reviews and Q&As

There are currently no Customer reviews or Questions for ab218610.
Please use the links above to contact us or submit feedback about this product.

Please note: All products are "FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC PROCEDURES, NOT FOR USE IN HUMANS"
For licensing inquiries, please contact partnerships@abcam.com

Sign up