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-19612B
    DDP-38003 trihydrochloride
    		Inhibitor
    DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
    DDP-38003 trihydrochloride
  • HY-141677A
    INCB059872 dihydrochloride
    		Inhibitor 99.18%
    INCB059872 dihydrochloride is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 dihydrochloride can be used for the research of myeloid leukemia.
    INCB059872 dihydrochloride
  • HY-119397A
    KDM5-C49 hydrochloride
    		Inhibitor 99.95%
    KDM5-C49 (KDOAM-20) hydrochloride is a potent and selective inhibitor of KDM5 demethylases, with IC50s of 40 nM, 160 nM, and 100 nM for KDM5A, KDM5B, and KDM5C enzymes, respectively. KDM5-C49 hydrochloride can be used for the research of cancer.
    KDM5-C49 hydrochloride
  • HY-138691A
    JQKD82 trihydrochloride
    		Inhibitor 99.94%
    JQKD82 (JADA82) trihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 trihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma.
    JQKD82 trihydrochloride
  • HY-139601
    KDM2B-IN-4
    		Inhibitor 99.59%
    KDM2B-IN-4 is a histone demethylase KDM2B inhibitor extracted from patent WO2016112284A1, compound 182b. KDM2B-IN-4 can be used for the research of cancer.
    KDM2B-IN-4
  • HY-132896
    KDM4-IN-3
    		Inhibitor 99.36%
    KDM4-IN-3 is a KDM4 inhibitor that exhibits improved potency in biochemical assays, is cell-permeable, and kills prostate cancer cells at low micromolar concentrations.
    KDM4-IN-3
  • HY-122635A
    T-448
    		Inhibitor 98.86%
    T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons.
    T-448
  • HY-112308
    NCGC00247743
    		Inhibitor 98.61%
    NCGC00247743 is a histone lysine demethylase KDM4 inhibitor.
    NCGC00247743
  • HY-139560
    KDM2B-IN-1
    		99.19%
    KDM2B-IN-1 is a histone demethylase (kdm2b) inhibitor and can be used for hyperproliferative diseases research.
    KDM2B-IN-1
  • HY-132198
    JMJD7-IN-1
    		Inhibitor 98.57%
    JMJD7-IN-1 is a potent JMJD7 inhibitor, with an IC50 of 6.62 μM. JMJD7-IN-1 shows good inhibitory activity against cells expressing a high level of JMJD7.
    JMJD7-IN-1
  • HY-123419
    CPI-4203
    		Inhibitor ≥99.0%
    CPI-4203 is a potent KDM5A inhibitor with an IC50 of 250 nM. CPI-4203 is competitive with 2-oxoglutarate (2-OG). CPI-4203 is structurally related to CPI-455 (HY-100421) but is less potent.
    CPI-4203
  • HY-15648C
    GSK-J5
    		Inhibitor 99.96%
    GSK-J5 is a potent inhibitor of Schistosome and worm. GSK-J5 increases schistosomula mortality and adult worm motility and mortality, as well as egg oviposition, in a dose- and time-dependent manner.
    GSK-J5
  • HY-113039
    L-2-Hydroxyglutaric acid
    		Inhibitor
    L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid 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
  • HY-149213
    LSD1-IN-24
    		Inhibitor 99.20%
    LSD1-IN-24(compound 3S) is a selective LSD1 inhibitor with IC50 = 0.247 μM. LSD1-IN-24 can mediate the expression of PD-L1, enhance T cell killing response, and can be used in cancer research.
    LSD1-IN-24
  • HY-123194
    SIRT2/6-IN-1
    		98.44%
    SIRT2/6-IN-1 (Compound 5) is a SIRT6/SIRT2 inhibitor, with IC50s of 106 μM and 114 μM. SIRT2/6-IN-1 increases H3K9 acetylation, increases glucose uptake and reduces TNF-α secretion in cells.
    SIRT2/6-IN-1
  • HY-19612A
    DDP-38003 dihydrochloride
    		Inhibitor 98.22%
    DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
    DDP-38003 dihydrochloride
  • HY-120766
    NCDM-32B
    		Inhibitor
    NCDM-32B is a potent and selective KDM4 inhibitor that impaires viability and transforming phenotypes of breast cancer.
    NCDM-32B
  • HY-145259
    HDAC6-IN-3
    		Inhibitor ≥98.0%
    HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor. HDAC6-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    HDAC6-IN-3
  • HY-110154
    NSC636819
    		≥98.0%
    NSC636819 is a competitive and selective inhibitor of KDM4A/KDM4B. KDM4A/KDM4B are potential progression factors for prostate cancer. NSC636819 has the potential for the research of cancer diseases, especially prostate cancer.
    NSC636819
  • HY-113038AS
    α-Hydroxyglutaric acid-13C5 disodium
    		99.80%
    α-Hydroxyglutaric acid-13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium 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-<sup>13</sup>C<sub>5</sub> disodium
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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