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-B0546A
    Procaine hydrochloride
    		99.90%
    Procaine hydrochloride is a DNA-demethylating agent. Procaine hydrochloride acts through multiple targets and has a slow onset and a short duration of action.
    Procaine hydrochloride
  • HY-100764
    YUKA1
    		Inhibitor 99.56%
    YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM, less active on KDM5C (IC50, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity.
    YUKA1
  • HY-109117
    Iadademstat
    		Inhibitor 99.61%
    Iadademstat (ORY-1001) is a highly potent, orally active and selective LSD1 (KDM1A) inhibitor with antileukemic activity. Iadademstat can be used for relapsed or refractory acute myeloid leukemia research.
    Iadademstat
  • HY-110154
    NSC636819
    		98.9%
    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-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-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-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-148807
    Zavondemstat
    		Inhibitor
    Zavondemstat (QC8222; TACH 101) is an inhibitor of histone lysine demethylase 4D (KDM4D) with antineoplastic activity.
    Zavondemstat
  • 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-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-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-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-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-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-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-136522
    S2116
    		Inhibitor 98.15%
    S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice.
    S2116
  • 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-162301
    P3FI-63
    		Inhibitor 98.35%
    P3FI-63 is a KDM3B inhibitor with a IC50 value of 7 μM. P3FI-63 has antitumor activity.
    P3FI-63
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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