2. Signaling Pathways
  3. Epigenetics
  4. Histone Demethylase

Histone Demethylase

Histone Demethylase

Related Products

PDF 1.04 MB

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-113038A
    α-Hydroxyglutaric acid disodium
    		Inhibitor ≥98.0%
    α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases.
    α-Hydroxyglutaric acid disodium
  • HY-139348
    PFI-90
    		Inhibitor 99.86%
    PFI-90 is a selective inhibitor of histone demethylase (KDM3B) that inhibits PAX3-FOXO1 action. PFI-90 induces apoptosis and myogenic differentiation, resulting in the cell death increased. PFI-90 has the potential for the antitumor activity. (patent WO2021101929A1).
    PFI-90
  • HY-151483
    TK-129
    		Inhibitor ≥98.0%
    TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease.
    TK-129
  • HY-109169C
    Bomedemstat dihydrochloride
    		Inhibitor 99.55%
    Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.
    Bomedemstat dihydrochloride
  • HY-108706
    KDM2A/7A-IN-1
    		Inhibitor 99.94%
    KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases.
    KDM2A/7A-IN-1
  • HY-112623
    Vafidemstat
    		Inhibitor 99.53%
    Vafidemstat (ORY-2001) is an oral, brain penetrant, dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor.
    Vafidemstat
  • HY-162275
    JMJD1C-IN-1
    		Inhibitor 99.99%
    JMJD1C-IN-1 (compound 193D7) is an inhibitor of JMJD1C with oral activity. JMJD1C-IN-1 targets tumor Treg cells without affecting systemic immune homeostasis.
    JMJD1C-IN-1
  • HY-15221
    Methylstat
    		Inhibitor 98.85%
    Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis.
    Methylstat
  • HY-100422
    KDM5-IN-1
    		Inhibitor 99.52%
    KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
    KDM5-IN-1
  • 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-W017132
    2,4-PDCA
    		Inhibitor 99.80%
    2,4-PDCA (2,4 pyridine dicarboxylic acid) is a broad-spectrum inhibitor of 2OG oxygenase, including JmjC domain-containing family of histone demethylases (JHDMs). 2,4-PDCA is a target chemical in the field of bio-based plastics.
    2,4-PDCA
  • HY-138830
    TAK-418
    		Inhibitor 99.81%
    TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM. TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models.
    TAK-418
  • HY-139434
    JMJD6-IN-1
    		Inhibitor 99.69%
    JMJD6-IN-1 (Compound 1-3) is a JMJD6 inhibitor, with an inhibition rate of 82% at 10 μM. JMJD6-IN-1 inhibits MCF-7 and HCC4006 cell proliferation with IC50s of 19.2 μM and 25.2 μM. JMJD6-IN-1 can be used for research of cancers.
    JMJD6-IN-1
  • HY-101451
    PBIT
    		Inhibitor 99.46%
    PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1) histone demethylase with an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with IC50s of 6 μM and 4.9 μM, respectively.
    PBIT
  • HY-107573
    KDM2/7-IN-1
    		Inhibitor 99.00%
    KDM2/7-IN-1 (TC-E 5002) is a selective histone demethylase KDM2/7 subfamily inhibitor (IC50 values are 0.2, 1.2, 6.8, 55, 83, >100 and >120 μM for KDM7A, KDM7B, KDM2A, KDM5A, KDM4C, KDM6A and KDM4A respectively). KDM2/7-IN-1 inhibits growth of HeLa and KYSE-150 cancer cells in vitro.
    KDM2/7-IN-1
  • HY-101928
    KDM4D-IN-1
    		Inhibitor 98.82%
    KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM.
    KDM4D-IN-1
  • HY-19333
    OG-L002
    		Inhibitor 99.81%
    OG-L002 is a potent and highly selective LSD1 inhibitor with an IC50 of 0.02 μM. OG-L002 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 potently inhibits the expression of HSV IE genes.
    OG-L002
  • 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-139561
    KDM2B-IN-2
    		99.36%
    KDM2B-IN-2, a potent histone demethylase (kdm2b) inhibitor with an IC50 of 0.021 μM in a KDM2B TR-FRET assay. KDM2B-IN-2 can be used for hyperproliferative diseases research.
    KDM2B-IN-2
  • HY-110130
    RN-1 dihydrochloride
    		Inhibitor 99.13%
    RN-1 dihydrochloride is a potent, brain-penetrant, irreversible and selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 70 nM. RN-1 dihydrochloride exhibits selectivity for LSD1 over MAO-A and MAO-B with IC50 values of 0.51 μM and 2.785 μM respectively.
    RN-1 dihydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.