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HDAC

Histone deacetylase (HDAC) inhibitors block enzymes that remove acetyl groups from histones and other proteins. Deacetylation compacts chromatin and generally represses transcription, so HDAC inhibitors are widely used to study gene regulation. Trichostatin A was characterized in 1990 as a specific inhibitor of mammalian histone deacetylase. The first mammalian HDAC was cloned in 1996 and found to be related to the yeast transcriptional regulator Rpd3p. Isoform-selective tools include entinostat for HDAC1 and HDAC3, and Tubastatin A HCl for HDAC6, a microtubule-associated deacetylase. Broad-spectrum hydroxamates such as vorinostat and panobinostat, together with the cyclic depsipeptide romidepsin, complete the range.

2 Items

  • AR420626
    Cat. No.
    A23991
    CAS No.
    1798310-55-0

    AR420626

    AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes.

    In stock View Details
    5 mg
    $77.00
    10 mg
    $132.00
    All 4 sizes
  • Triciferol
    Cat. No.
    A24009
    CAS No.
    957214-00-5

    Triciferol

    Triciferol is a multifunctional small molecule that acts as both a vitamin D receptor (VDR) agonist and a histone deacetylase (HDAC) antagonist. It binds directly to VDR with an IC₅₀ of 87 nM and exhibits 1,25-dihydroxyvitamin D₃ (1,25D)-like potency in activating multiple VDR target genes. In addition to its transcriptional effects, Triciferol induces significant tubulin hyperacetylation and enhances histone acetylation, contributing to its antiproliferative and cytotoxic activities. This dual mechanism highlights its potential as a therapeutic agent in cancer and epigenetic modulation.

    In stock View Details
    1 mg
    $468.00
    5 mg
    $1,404.00
    All 4 sizes

2 Items

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