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-176283
    Tubulin/LSD1-IN-1
    		Inhibitor
    Tubulin/LSD1-IN-1 is an effective dual inhibitor of Tubulin polymerization and LSD1 (IC50 = 1.72 μM). Tubulin/LSD1-IN-1 has broad-spectrum antiproliferative activity against cancer cell lines. Tubulin/LSD1-IN-1 inhibits tubulin polymerization by targeting colchicine binding sites, thereby disrupting the microtubule network in gastric cancer cells. Tubulin/LSD1-IN-1 increases the methylation levels of H3K4me1/2 and H3K9me2/3, thereby achieving epigenetic regulation. Tubulin/LSD1-IN-1 induces G2/M arrest, promotes apoptosis, and effectively inhibits colony formation of gastric cancer cells.
    Tubulin/LSD1-IN-1
  • HY-144757
    LSD1-IN-16
    		Inhibitor
    LSD1-IN-16 (compound 4b) is a potent LSD1 inhibitor. LSD1-IN-16 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.015, 0.024, and 0.366 μM, respectively. LSD1-IN-16 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 15.2 μM.
    LSD1-IN-16
  • HY-103641R
    (2R)-Octyl-α-hydroxyglutarate (Standard)
    		Inhibitor
    (2R)-Octyl-α-hydroxyglutarate (Standard) is the analytical standard of (2R)-Octyl-α-hydroxyglutarate. This product is intended for research and analytical applications. (2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) is a modified form of D-isomer 2-Hydroxyglutarate.
    (2R)-Octyl-α-hydroxyglutarate (Standard)
  • HY-129388C
    Pulrodemstat hydrochloride
    		Inhibitor
    Pulrodemstat (CC-90011) hydrochloride is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 value of 0.25 nM. Pulrodemstat hydrochloride is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat hydrochloride induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
    Pulrodemstat hydrochloride
  • HY-17447SA
    Tranylcypromine-d5 hydrochloride
    		Inhibitor
    Tranylcypromine-d5 (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis.
    Tranylcypromine-d<sub>5</sub> hydrochloride
  • HY-15648G
    GSK-J1 sodium
    		Inhibitor
    GSK-J1 sodium is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 value of 60 nM towards KDM6B.
    GSK-J1 sodium
  • HY-173590
    AW4
    		Inhibitor
    AW4 is a LSD1 inhibitor. AW4 inhibits LSD1 ΔTTAS activity in H3K4me2 demethylation assays. AW4 can be used for research of drug resistance.
    AW4
  • HY-162955
    LSD1/HDAC-IN-1
    		Inhibitor
    LSD1/HDAC-IN-1 (compound 2) is a potent inhibitor of HDAC and LSD1, with IC50s of 0.125 nM, 0.373 nM, 0.0118 nM, 0.103 nM, and 0.571 μM for HDAC1, HDAC2, HDAC6, HDAC8 and LSD1, respectively. LSD1/HDAC-IN-1 plays an important role in cancer research.
    LSD1/HDAC-IN-1
  • HY-W744986
    L-2-Hydroxyglutaric acid-d5 disodium
    L-2-Hydroxyglutaric acid-d5 disodium ((2S)-2-Hydroxyglutaric acid-d5 disodium) is the deuterium labeled L-2-Hydroxyglutaric acid disodium (HY-W015114). L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium 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-d<sub>5</sub> disodium
  • HY-138691
    JQKD82
    		Inhibitor
    JQKD82 (JADA82) is a cell-permeable and selective KDM5 inhibitor. JQKD82 increases H3K4me3 and can be used for the research of multiple myeloma.
    JQKD82
  • HY-146440
    LSD1/ER-IN-1
    		Inhibitor
    LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC50 of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC50 of 8.79 μM.
    LSD1/ER-IN-1
  • HY-168504
    LSD1-IN-36
    		Inhibitor
    LSD1-IN-36 is a potent LSD1 inhibitor with an IC50 value of 0.8 nM. LSD1-IN-36 induces apoptosis and arrests the cell cycle. LSD1-IN-36 shows antitumor activity.
    LSD1-IN-36
  • HY-15774A
    CBB1003 hydrochloride
    		Inhibitor
    CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.
    CBB1003 hydrochloride
  • HY-15648BR
    GSK-J4 (Standard)
    		Inhibitor
    GSK-J4 (Standard) is the analytical standard of GSK-J4. This product is intended for research and analytical applications. GSK-J4 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 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.
    GSK-J4 (Standard)
  • HY-B1496R
    Tranylcypromine hemisulfate (Standard)
    		Inhibitor
    Tranylcypromine (hemisulfate) (Standard) is the analytical standard of Tranylcypromine (hemisulfate). This product is intended for research and analytical applications. Tranylcypromine (SKF 385) hemisulfate is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hemisulfate is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis. Tranylcypromine has antidepressant effects.
    Tranylcypromine hemisulfate (Standard)
  • HY-138691B
    JQKD82 dihydrochloride
    		Inhibitor
    JQKD82 (JADA82) dihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 dihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma.
    JQKD82 dihydrochloride
  • HY-160183
    LSD1-IN-29
    		Inhibitor
    LSD1-IN-29 (compound 6) is a Lysine specific demethylase 1 (LSD1) inhibitor with the IC50 of 19 nM.
    LSD1-IN-29
  • HY-159901
    LSD1-IN-37
    		Inhibitor
    LSD1-IN-37 (Compound 5g) is a lysine-specific demethylase 1 (LSD1) inhibitor constructed using an efficient synthesis strategy incorporating hexafluoroisopropyl groups. This metal-free method exhibits excellent reaction stability and adaptability. LSD1-IN-37 demonstrated outstanding LSD1 inhibitory activity and holds potential for further research.
    LSD1-IN-37
  • HY-119730
    Tripartin
    		Inhibitor
    Tripartin is an inhibitor of histone demethylase. Tripartin inhibits the histone H3 lysine 9 demethylase KDM4 in HeLa cells.
    Tripartin
  • HY-157408
    KDM4D-IN-3
    KDM4D-IN-3 (compound 1) is a small-molecule epigenetic inhibitor target at KDM4D with an IC50 value of 4.8 μM.
    KDM4D-IN-3
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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