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    unc1999-ezh2-methyltransferase-inhibitor-ab146152.pdf

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Epigenetics and Nuclear Signaling Chromatin Modifying Enzymes Methylation
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UNC1999, EZH2 methyltransferase inhibitor (ab146152)

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Key features and details

  • Potent, selective cell-permeable EZH2 methyltransferase inhibitor
  • CAS Number: 1431612-23-5
  • Purity: > 98%
  • Soluble in DMSO (up to 10 mg/ml)

  • Form / State: Solid
  • Source: Synthetic

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Overview

  • Product name

    UNC1999, EZH2 methyltransferase inhibitor
  • Description

    Potent, selective cell-permeable EZH2 methyltransferase inhibitor
  • Biological description

    Potent, selective cell-permeable dual inhibitor of EZH2 and EZH1 methyltransferase inhibitor (IC50 = 45 nM and 2 nM respectively) (Konze et al. ). Inhibits H3K27 methylation (IC50 = 124 nM, MCF10A cells). Competitive with the cofactor SAM, and non-competitive with the peptide substrate. Inhibition of EZH2 with UNC1999 enhanced the efficacy of gefitinib in suppressing the proliferation of colon cancer cells (Katona et al.). It suppresses global H3K27 trimethylation/demethylation and inhibits the growth of mixed lineage leukemia (MLL)-rearranged leukemia cells ( Xu et al.).  Orally bioavailable.

  • Purity

    > 98%
  • CAS Number

    1431612-23-5
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    N-[(6-Methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4-carboxamide

  • Molecular weight

    569.74
  • Molecular formula

    C33H43N7O2
  • PubChem identifier

    72551585
  • Storage instructions

    Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
  • Solubility overview

    Soluble in DMSO (up to 10 mg/ml)

  • 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=CN=C(C=C4)N5CCN(CC5)C(C)C)C(C)C
  • Source

    Synthetic

  • Research areas

    • Epigenetics and Nuclear Signaling
    • Chromatin Modifying Enzymes
    • Methylation
    • Epigenetics and Nuclear Signaling
    • Chromatin Remodeling
    • Polycomb Silencing
    • PRC2
    • Epigenetics and Nuclear Signaling
    • Chromatin Remodeling
    • Polycomb Silencing
    • PRC3
    • Epigenetics and Nuclear Signaling
    • Chromatin Modifying Enzymes
    • Methylation
    • Lysine methylation
    • Cancer
    • Tumor biomarkers
    • Enzymes
    • Other
    • Biochemicals
    • Product Range
    • New
    • Biochemicals
    • Chemical Type
    • Biochemicals
    • Biochemicals
    • Pharmacology
    • Signaling
    • Epigenetics
    • Histone Methyltransferase (HMT)
    • Biochemicals
    • Pharmacology
    • Enzymes
    • Transferase
    • Histone Methyltransferase (HMT)
    • Histone lysine methyltransferase (KMT)

Associated products

    Protocols

    To our knowledge, customised protocols are not required for this product. Please try the standard protocols listed below and let us know how you get on.

    Click here to view the general protocols

    Datasheets and documents

    • SDS download

    • Datasheet download

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    References (0)

    Publishing research using ab146152? Please let us know so that we can cite the reference in this datasheet.

    ab146152 has not yet been referenced specifically in any publications.

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