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-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-15648FR
    GSK-J4 hydrochloride (Standard)
    		Inhibitor
    GSK-J4 (hydrochloride) (Standard) is the analytical standard of GSK-J4 (hydrochloride). This product is intended for research and analytical applications. GSK-J4 hydrochloride 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 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1.
    GSK-J4 hydrochloride (Standard)
  • 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-175184
    LSD1-IN-44
    		Inhibitor
    LSD1-IN-44 (Compound 19) is a LSD1 inhibitor with an IC50 of 0.02  μM for LSD1-CoREST enzymatic complex. LSD1-IN-44 has significant antischistosomal activity against transformed schistosomula (NTS) and Schistosoma mansoni adult worms while showing a delayed onset of action towards juvenile forms. LSD1-IN-44 has no significant toxicity to human cells. LSD1-IN-44 can be used for schistosomiasis research.
    LSD1-IN-44
  • HY-175185
    MC3935
    		Inhibitor
    MC3935 is a LSD1 inhibitor with an IC50 of 0.52  μM for LSD1-CoREST enzymatic complex. MC3935 has significant antischistosomal activity against transformed schistosomula (NTS) and Schistosoma mansoni adult worms while showing a delayed onset of action towards juvenile forms. MC3935 has no significant toxicity to human cells. MC3935 can be used for schistosomiasis research.
    MC3935
  • 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-12315R
    N-Oxalylglycine (Standard)
    		Inhibitor
    N-Oxalylglycine (Standard) is the analytical standard of N-Oxalylglycine. This product is intended for research and analytical applications. N-Oxalylglycine (N-Oxaloglycine) is a Jumonji C-domain-containing histone lysine demethylase inhibitor. N-Oxalylglycine inhibits JMJD2A, JMJD2C and JMJD2D. N-Oxalylglycine also inhibits HIF prolylhydroxylase domain-1 (PHD-1) and PHD-2, with an IC50 of 2.1 μM and 5.6 μM, respectively.
    N-Oxalylglycine (Standard)
  • 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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