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-17447SA
    Tranylcypromine-d5 hydrochloride
    		Inhibitor
    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[1][2].
    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-113038AS1
    α-Hydroxyglutaric acid-d4 disodium
    α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
    α-Hydroxyglutaric acid-d<sub>4</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-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-15774A
    CBB1003 hydrochloride
    		Inhibitor
    CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.
    CBB1003 hydrochloride
  • 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-160183
    LSD1-IN-29
    		Inhibitor
    LSD1-IN-29 (compound 6) is a Lysine specific demethylase 1 (LSD1) inhibitor with the IC50 of 19 nM.
    LSD1-IN-29
  • HY-119730
    Tripartin
    		Inhibitor
    Tripartin is an inhibitor of histone demethylase. Tripartin inhibits the histone H3 lysine 9 demethylase KDM4 in HeLa cells.
    Tripartin
  • HY-157408
    KDM4D-IN-3
    KDM4D-IN-3 (compound 1) is a small-molecule epigenetic inhibitor target at KDM4D with an IC50 value of 4.8 μM.
    KDM4D-IN-3
  • HY-13643R
    Daminozide (Standard)
    		Inhibitor
    Daminozide (Standard) is the analytical standard of Daminozide. This product is intended for research and analytical applications. Daminozide, a plant growth regulator, is a selective inhibitor of the human KDM2/7 histone demethylases, with IC50s of 0.55, 1.5 and 2.1 μM for PHF8, KDM2A, and KIAA1718, respectively. Daminozide has >100-fold selectivity for KDM2/7 subfamily versus other demethylase subfamily members tested.
    Daminozide (Standard)
  • HY-15774
    CBB1003
    		Inhibitor
    CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.
    CBB1003
  • HY-161848
    TCP-MP-CA
    		Inhibitor
    TCP-MP-CA (compound 11a) is an inhibitor of LSD1 demethylation enzymatic via binding to LSD1/CoREST complex. TCP-MP-CA exhibits an inhibitory effect on osteoclastogenesis, with an IC50 value of 0.14 µM.
    TCP-MP-CA
  • HY-19333A
    OG-L002 hydrochloride
    		Inhibitor
    OG-L002 hydrochloride is a potent and highly selective LSD1 inhibitor with an IC50 of 0.02 μM. OG-L002 hydrochloride is a potent monoamine oxidases (MAO) inhibitor with IC50s of 1.38 μM and 0.72 μM for MAO-A and MAO-B, respectively. OG-L002 hydrochloride potently inhibits the expression of HSV IE genes.
    OG-L002 hydrochloride
  • HY-B0660R
    Eicosapentaenoic Acid (Standard)
    		Activator
    Eicosapentaenoic Acid (Standard) is the analytical standard of Eicosapentaenoic Acid. This product is intended for research and analytical applications. 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 (Standard)
  • HY-15648D
    GSK-J1 lithium salt
    		Inhibitor 98.26%
    GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
    GSK-J1 lithium salt
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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