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-103085R
    T-3775440 hydrochloride (Standard)
    		Inhibitor
    T-3775440 hydrochloride (Standard) is the analytical standard of T-3775440 hydrochloride (HY-103085). This product is intended for research and analytical applications. T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM.
    T-3775440 hydrochloride (Standard)
  • HY-100422R
    KDM5-IN-1 (Standard)
    		Inhibitor
    KDM5-IN-1 (Standard) is the analytical standard of KDM5-IN-1 (HY-100422). This product is intended for research and analytical applications. KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
    KDM5-IN-1 (Standard)
  • HY-100546AR
    GSK-LSD1 dihydrochloride (Standard)
    		Inhibitor
    GSK-LSD1 (dihydrochloride) (Standard) is the analytical standard of GSK-LSD1 (dihydrochloride) (HY-100546A). This product is intended for research and analytical applications. GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.
    GSK-LSD1 dihydrochloride (Standard)
  • 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-100014R
    KDM5A-IN-1 (Standard)
    		Inhibitor
    KDM5A-IN-1 (Standard) is the analytical standard of KDM5A-IN-1 (HY-100014). This product is intended for research and analytical applications. 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).
    KDM5A-IN-1 (Standard)
  • 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)
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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