1. Signaling Pathways
  2. Epigenetics
  3. 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 (46):

Cat. No. Product Name Effect Purity
  • HY-15648B
    GSK-J4 Inhibitor >98.0%
    GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable prodrug of GSK-J1.
  • HY-104048
    QC6352 Inhibitor >98.0%
    QC6352 is a potent KDM4C inhibitor with an IC50 of 35 nM.
  • HY-18632
    GSK2879552 Inhibitor 99.94%
    GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
  • HY-12635
    SP2509 Antagonist 99.81%
    SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with IC50 of 13 nM.
  • HY-100421
    CPI-455 Inhibitor >98.0%
    CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
  • HY-116761
    GSK467 Inhibitor 99.20%
    GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM, shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members.
  • HY-122635A
    T-448 Inhibitor 98.86%
    T-448 is a specific and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons.
  • HY-102047B
    KDOAM-25 citrate Inhibitor 98.04%
    KDOAM-25 citrate is a potent and highly selective KDM5 sub-family of histone lysine demethylases inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.
  • HY-12782T
    ORY-1001(trans) Inhibitor 99.14%
    ORY-1001 trans is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
  • HY-B1496
    Tranylcypromine hemisulfate Inhibitor 99.05%
    Tranylcypromine hemisulfate is an irreversible, nonselective MAO inhibitor used in the treatment of depression.
  • 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-103713
    Seclidemstat Inhibitor 98.78%
    Seclidemstat (SP-2577) is a potent and orally bioavailable LSD1 inhibitor, with a mean IC50 of 127 nM.
  • HY-101799
    NCGC00244536 Inhibitor 98.57%
    NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM.
  • HY-15648
    GSK-J1 Inhibitor 99.98%
    GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B. 
  • HY-12304
    IOX1 Inhibitor
    IOX1, 5-Carboxy-8-hydroxyquinoline, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC50 values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively.
  • HY-13953
    JIB-04 Inhibitor 98.39%
    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-13643
    Daminozide Inhibitor >98.0%
    Daminozide(DMASA; DIMG; B 995), a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.
  • 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-100014
    KDM5A-IN-1 Inhibitor 98.65%
    KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
  • HY-12725
    ML324 Inhibitor >98.0%
    ML324 is a potent JMJD2 demethylase inhibitor with demonstrated antiviral activity.
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