1. Epigenetics
  2. Histone Demethylase

Histone Demethylase

There are two classes of enzymes involved in histone methylation: methyltransferases and demethylases. While methyltransferases are responsible for establishing methylation patterns, demethylases are capable of removing methyl groups not only from histones but other proteins as well. Histone demethylases not only target methylated sites on histone tails but also interact with methylated sites on non-histone proteins, such as p53.

Histone lysine demethylases (KDMs) are of interest as drug targets due to their regulatory roles in chromatin organization and their tight associations with diseases including cancer and mental disorders.

JMJD1A (also named KDM3A) is a demethylasethat removes methyl from histone lysine H3K9. It plays important roles in various cellular processes, including spermatogenesis, energy metabolism, regulation of stem cell and gender display.

Jumonji domain-containing 3 (Jmjd3) has been identified as a histone demethylase, which specifically catalyzes the removal of methylation from H3K27me3.

Histone Demethylase Related Products (20):

Cat. No. Product Name Effect Purity
  • HY-15648B
    GSK-J4 Inhibitor
    GSK J4 is a cell permeable prodrug rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor; attenuates lipopolysaccharide (LPS)-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 μM for the inhibition of TNFα release).
  • HY-18632
    GSK2879552 Inhibitor 99.82%
    GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
  • HY-12635
    SP2509 Antagonist 99.38%
    SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with IC50 of 13 nM.
  • HY-15648
    GSK-J1 Inhibitor 99.90%
    GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
  • HY-B1496
    Tranylcypromine hemisulfate Inhibitor 99.82%
    Tranylcypromine hemisulfate, an LSD1 inhibitor, and also an irreversible, nonselective MAO inhibitor, is used in the treatment of depression.
  • HY-100421
    CPI-455 Inhibitor >98.0%
    CPI-455 is a specific KDM5 inhibitor.
  • HY-19612A
    DDP-38003 dihydrochloride Inhibitor
    DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
  • HY-12782
    ORY-1001 Inhibitor >98.0%
    ORY-1001 (RG-6016) is a potent LSD1 inhibitor extracted from patent WO2013057322A1.
  • HY-13953
    JIB-04 Inhibitor
    JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
  • HY-12725
    ML324 Inhibitor 98.19%
    ML324 is a potent JMJD2 demethylase inhibitor with demonstrated antiviral activity.
  • HY-12304
    IOX1 Inhibitor
    IOX1 is the most potent broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases; IC50 for KDM4A/KDM3A is 0.6/0.1 uM.
  • HY-15648A
    GSK-J2 Inhibitor 98.82%
    GSK-J2 is a pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 (IC50 > 100 μM), making it an appropriate negative control for in vitro studies involving GSK-J1; GSK-J1 is a selective inhibitor for human H3K27me3 demethylases.
  • HY-13643
    Daminozide Inhibitor
    Daminozide(DMASA; DIMG; B 995), a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.
  • HY-100014
    KDM5A-IN-1 Inhibitor 99.76%
    KDM5A-IN-1 is an inhibitor histone demethylases.
  • HY-15313B
    CBB1007 hydrochloride Inhibitor
    CBB1007 Hcl is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
  • HY-15313C
    CBB1007 trihydrochloride Inhibitor
    CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
  • HY-15313
    CBB1007 Inhibitor
    CBB1007 is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
  • HY-15648D
    GSK-J1 lithium salt Inhibitor
    GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
  • HY-15774A
    CBB1003 hydrochloride Inhibitor
    CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
  • HY-15774
    CBB1003 Inhibitor
    CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.