2. Signaling Pathways
  3. Epigenetics
  4. Histone Demethylase

Histone Demethylase

Histone Demethylase

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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 Isoform Specific Products:

Histone Demethylase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-103641R
    (2R)-Octyl-α-hydroxyglutarate (Standard)
    		Inhibitor
    (2R)-Octyl-α-hydroxyglutarate (Standard) is the analytical standard of (2R)-Octyl-α-hydroxyglutarate. This product is intended for research and analytical applications. (2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) is a modified form of D-isomer 2-Hydroxyglutarate.
    (2R)-Octyl-α-hydroxyglutarate (Standard)
  • HY-129388C
    Pulrodemstat hydrochloride
    		Inhibitor
    Pulrodemstat (CC-90011) hydrochloride is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 value of 0.25 nM. Pulrodemstat hydrochloride is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat hydrochloride induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
    Pulrodemstat hydrochloride
  • HY-17447SA
    Tranylcypromine-d5 hydrochloride
    		Inhibitor 99.42%
    Tranylcypromine-d5 (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis.
    Tranylcypromine-d<sub>5</sub> hydrochloride
  • HY-15648G
    GSK-J1 sodium
    		Inhibitor
    GSK-J1 sodium is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 value of 60 nM towards KDM6B.
    GSK-J1 sodium
  • HY-173590
    AW4
    		Inhibitor
    AW4 is a LSD1 inhibitor. AW4 inhibits LSD1 ΔTTAS activity in H3K4me2 demethylation assays. AW4 can be used for research of drug resistance.
    AW4
  • HY-162955
    LSD1/HDAC-IN-1
    		Inhibitor
    LSD1/HDAC-IN-1 (compound 2) is a potent inhibitor of HDAC and LSD1, with IC50s of 0.125 nM, 0.373 nM, 0.0118 nM, 0.103 nM, and 0.571 μM for HDAC1, HDAC2, HDAC6, HDAC8 and LSD1, respectively. LSD1/HDAC-IN-1 plays an important role in cancer research.
    LSD1/HDAC-IN-1
  • HY-W744986
    L-2-Hydroxyglutaric acid-d5 disodium
    L-2-Hydroxyglutaric acid-d5 disodium ((2S)-2-Hydroxyglutaric acid-d5 disodium) is the deuterium labeled L-2-Hydroxyglutaric acid disodium (HY-W015114). L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively.
    L-2-Hydroxyglutaric acid-d<sub>5</sub> disodium
  • HY-138691
    JQKD82
    		Inhibitor
    JQKD82 (JADA82) is a cell-permeable and selective KDM5 inhibitor. JQKD82 increases H3K4me3 and can be used for the research of multiple myeloma.
    JQKD82
  • HY-B0660S1
    Eicosapentaenoic acid 1,2,3,4,5-13C5
    		Activator
    Eicosapentaenoic acid 1,2,3,4,5-13C5 (EPA 1,2,3,4,5-13C, FA 20:5-13C5) is 13C labeled Eicosapentaenoic Acid. Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation.
    Eicosapentaenoic acid 1,2,3,4,5-<sup>13</sup>C<sub>5</sub>
  • HY-146440
    LSD1/ER-IN-1
    		Inhibitor
    LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC50 of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC50 of 8.79 μM.
    LSD1/ER-IN-1
  • HY-168504
    LSD1-IN-36
    		Inhibitor
    LSD1-IN-36 is a potent LSD1 inhibitor with an IC50 value of 0.8 nM. LSD1-IN-36 induces apoptosis and arrests the cell cycle. LSD1-IN-36 shows antitumor activity.
    LSD1-IN-36
  • HY-15774A
    CBB1003 hydrochloride
    		Inhibitor
    CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.
    CBB1003 hydrochloride
  • HY-15648BR
    GSK-J4 (Standard)
    		Inhibitor
    GSK-J4 (Standard) is the analytical standard of GSK-J4. This product is intended for research and analytical applications. 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 proagent of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.
    GSK-J4 (Standard)
  • HY-108706R
    KdM2A/7A-IN-1 (Standard)
    		Inhibitor
    KdM2A/7A-IN-1 (Standard) is the analytical standard of KdM2A/7A-IN-1 (HY-108706). This product is intended for research and analytical applications. KdM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KdM2A/7A, with an IC50 of 0.16 μM for KdM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases.
    K<sub>d</sub>M2A/7A-IN-1 (Standard)
  • HY-101928R
    KDM4D-IN-1 (Standard)
    		Inhibitor
    KDM4D-IN-1 (Standard) is the analytical standard of KDM4D-IN-1 (HY-101928). This product is intended for research and analytical applications. KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM.
    KDM4D-IN-1 (Standard)
  • HY-B1496R
    Tranylcypromine hemisulfate (Standard)
    		Inhibitor
    Tranylcypromine (hemisulfate) (Standard) is the analytical standard of Tranylcypromine (hemisulfate). This product is intended for research and analytical applications. Tranylcypromine (SKF 385) hemisulfate is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hemisulfate is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis. Tranylcypromine has antidepressant effects.
    Tranylcypromine hemisulfate (Standard)
  • HY-100764R
    YUKA1 (Standard)
    		Inhibitor
    YUKA1 (Standard) is the analytical standard of YUKA1 (HY-100764). This product is intended for research and analytical applications. YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM. YUKA1 has less inhibitory active on KDM5C (IC50 = 7.12 μM) and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 can increase H3K4me3 levels and inhibit cell proliferation. YUKA1 can be used for the research of cancer, such as lung and breast cancers.
    YUKA1 (Standard)
  • HY-101799R
    NCGC00244536 (Standard)
    		Inhibitor
    NCGC00244536 (Standard) (KDM4B Inhibitor B3 (Standard)) is the analytical standard of NCGC00244536 (HY-101799). This product is intended for research and analytical applications. NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM.
    NCGC00244536 (Standard)
  • HY-138691B
    JQKD82 dihydrochloride
    		Inhibitor
    JQKD82 (JADA82) dihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 dihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma.
    JQKD82 dihydrochloride
  • HY-183928
    EPZ020809
    		Inhibitor
    EPZ020809 is a competitive KDM4C inhibitor with a Ki of 31 nM.
    EPZ020809
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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