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 (31):

Cat. No. Product Name Effect Purity
  • HY-15648B
    GSK-J4 Inhibitor >98.0%
    GSK-J4 is a potent H3K27me3 demethylase inhibitor, with IC50s of 8.6 µM and 6.6 µM towards KDM6B and KDM6A respectively.
  • HY-12635
    SP2509 Antagonist 98.92%
    SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with IC50 of 13 nM.
  • HY-18632
    GSK2879552 Inhibitor 99.82%
    GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
  • 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-12782
    ORY-1001(mixture of trans and cis isomers) Inhibitor >98.0%
    ORY-1001(mixture of trans and cis isomers) is a potent LSD1 inhibitor extracted from patent WO2013057322A1, Compound Example 1, has an IC50 of 17 nM.
  • HY-112308
    NCGC00247743 Inhibitor
    NCGC00247743 is a histone lysine demethylase KDM4 inhibitor.
  • HY-12782T
    ORY-1001(trans) Inhibitor 99.14%
    ORY-1001 trans is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
  • HY-103713
    Seclidemstat Inhibitor 98.78%
    Seclidemstat is a potent LSD1 inhibitor, with a mean IC50 of 127 nM.
  • HY-104048
    QC6352 Inhibitor >98.0%
    QC6352 is a potent KDM4C inhibitor with an IC50 of 35 nM.
  • HY-15648
    GSK-J1 Inhibitor 99.92%
    GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B. 
  • HY-12725
    ML324 Inhibitor >98.0%
    ML324 is a potent JMJD2 demethylase inhibitor with demonstrated antiviral activity.
  • HY-100421
    CPI-455 Inhibitor >98.0%
    CPI-455 is a specific KDM5 inhibitor.
  • 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-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-101799
    NCGC00244536 Inhibitor 98.57%
    NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM.
  • HY-100422
    KDM5-IN-1 Inhibitor >98.0%
    KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
  • HY-100546A
    GSK-LSD1 Dihydrochloride Inhibitor >98.0%
    GSK-LSD1 Dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.
  • HY-100014
    KDM5A-IN-1 Inhibitor 99.76%
    KDM5A-IN-1 is an inhibitor histone demethylases.
  • HY-13643
    Daminozide Inhibitor >98.0%
    Daminozide(DMASA; DIMG; B 995), a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.
  • HY-19612B
    DDP-38003 trihydrochloride Inhibitor 98.74%
    DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.