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-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-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-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-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-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-159901
    LSD1-IN-37
    		Inhibitor
    LSD1-IN-37 (Compound 5g) is a lysine-specific demethylase 1 (LSD1) inhibitor constructed using an efficient synthesis strategy incorporating hexafluoroisopropyl groups. This metal-free method exhibits excellent reaction stability and adaptability. LSD1-IN-37 demonstrated outstanding LSD1 inhibitory activity and holds potential for further research.
    LSD1-IN-37
  • 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-168527
    Acaricide agent 1
    		Inhibitor
    Acaricide agent 1 (Compound 7l) is a potent LSD1 inhibitor. LSD1 exhibits excellent acaricidal activity against egg of T. cinnabarinus with a LC50 of 0.0035 mg/L.
    Acaricide agent 1
  • 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-B0660A
    Eicosapentaenoic acid (metformin)
    		Activator
    Eicosapentaenoic Acid (EPA) metformin is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic acid metformin exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). EEicosapentaenoic acid metformin activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic acid metformin can promote relaxation of vascular smooth muscle cells and vasodilation.
    Eicosapentaenoic acid (metformin)
  • 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-169919
    HDM-IN-1
    		Inhibitor
    HDM-IN-1 (Compound A4) is an inhibitor for fungal histone demethylase (HDM), that inhibits the H3K27me3 in Cryptococcus neoformans and in Candida auris with IC50s of 134 and 12 nM. HDM-IN-1 exhibits inhibitory efficacy against C. neoformans and C. auris with MIC80 of 0.5-2 μg/mL, through inhibition of the biofilm and capsule formation. HDM-IN-1 exhibits antifungal activity in ICR mouse model.
    HDM-IN-1
  • 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>
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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