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Covalent modifications to DNA or histone proteins with various chemical groups can determine whether genes are turned on or off and can thus influence the production of proteins in a cell. This genetic control without altering DNA sequences is crucial in many normal cellular functions. Aberrant epigenetic alterations are present in myriad disease states. Pharmacological manipulation of the various enzymes involved in epigenetic changes in pathological states is an important new target in drug discovery. Writers (methyl and acetyl transferases) are enzymes capable of modifying nucleotide bases and amino acid residues on histones. Erasers (demethylases and deacetylases) remove these same modifications. Readers (bromodomains) are enzymes capable of recognizing specific epigenetic marks that direct a particular transcriptional outcome.

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  • Bromosporine

    Bromosporine is a pan-bromodomain inhibitor

  • I-BET762

    I-BET762 is a potent inhibitor of the BET family of bromodomains

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DNA Methylation

  • RG-108

    Non-nucleoside DNA methyltransferase inhibitor

  • Decitabine

    Decitabine is a DNA methyltransferase inhibitor

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Histone Deacetylation

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Histone Demethylation

  • SP2509

    SP2509 is a potent and reversible inhibitor of LSD1

  • ML324

    ML324 is an inhibitor of JMJD2 histone demethylases

  • CPI-455

    CPI-455 is a potent and selective inhibitor of the lysine demethylase KDM5

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Histone Methylation

  • (R)-PFI-2

    Potent and selective SAM-dependent inhibitor of the methyltransferase SETD7

  • A-196

    Potent and selective inhibitor of the methyltransferase SUV420H1/H2

  • EPZ015666

    Potent and selective inhibitor of the arginine methyltransferase PRMT5

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Histone Acetylation

  • Anacardic acid

    Anacardic acid is an inhibitor of the acetyltransferases p300 and PCAF

  • CPTH2

    CPTH2 is a selective inhibitor of the acetyl transferase Gcn5P

  • CTPB

    CTPB is a selective activator of the acetyltransferase p300. Selective over PCAF.

View All Histone Acetylation Reagents