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-151191
    LSD1-IN-22
    		Inhibitor
    LSD1-IN-22 is a potent Lysine-specific demethylase 1 (LSD1) inhibitor with a Ki value of 98 nM. LSD1-IN-22 has anti-proliferative activity against certain cancer cells.
    LSD1-IN-22
  • HY-W011269
    Eicosapentaenoic Acid sodium
    		Activator
    Eicosapentaenoic Acid (EPA)sodium is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid sodium exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid sodium activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid sodium can promote relaxation of vascular smooth muscle cells and vasodilation.
    Eicosapentaenoic Acid sodium
  • HY-158433
    KDM5B ligand 2
    KDM5B ligand 2 is the ligand for target protein KDM5B. KDM5B ligand 2 is utilized for synthesis of KDM5B PROTAC GT-653 (HY-158432).
    KDM5B ligand 2
  • HY-172170
    LSD1-IN-39
    		Inhibitor
    LSD1-IN-39 (Compound 14) is a reversible inhibitor for LSD1 with an IC50 of 0.18 μM. LSD1-IN-39 exhibits broad-spectrum anti-proliferative activity against cancer cells, inhibits the cell migration of HepG2 and inhibits the epithelial-mesenchymal transition. LSD1-IN-39 exhibits antitumor activity in mouse models.
    LSD1-IN-39
  • HY-146670
    KDM5B-IN-3
    		Inhibitor
    KDM5B-IN-3 (Compound 5) is a histone lysine specific demethylase 5B (KDM5B/JARID1B) inhibitor with an IC50 of 9.32 μM. KDM5B-IN-3 can be used for the research of gastric cancer.
    KDM5B-IN-3
  • HY-W704805
    Sodium 2-hydroxypentanedioate-2,3,3-d3
    Sodium 2-hydroxypentanedioate-2,3,3-d3 is the deuterium labeled α-Hydroxyglutaric acid disodium (HY-113038A). 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.
    Sodium 2-hydroxypentanedioate-2,3,3-d<sub>3</sub>
  • HY-146284
    LSD1-IN-19
    		Inhibitor
    LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.108 μM and KD of 0.068 μM, respectively. LSD1-IN-19 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.17 and 0.40 μM, respectively.
    LSD1-IN-19
  • HY-149946
    HDAC-IN-57
    		Inhibitor
    HDAC-IN-57 is an orally active inhibitor of histone deacetylases (HDAC), with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC50 of 1.34 μΜ. HDAC-IN-57 induces apoptosis, and has anti-tumor activity.
    HDAC-IN-57
  • HY-172809
    LSD1-IN-42
    		Inhibitor
    LSD1-IN-42 (Compound 7ae) is an orally active LSD1 inhibitor that potently inhibits LSD1 activity (IC50 = 0.08 μM). LSD1-IN-42 downregulates PD-L1 expression and enhances T cell-mediated tumor killing effects. LSD1-IN-42 demonstrates significant anti-gastric cancer activity by inhibiting tumor cell invasion and migration.
    LSD1-IN-42
  • HY-138830A
    (S,S)-TAK-418
    		Inhibitor
    (S,S)-TAK-418 is a potent inhibitor of lysine-specific demethylase 1 (LSD1), demonstrating significant normalization of aberrant gene expression in neurodevelopmental disorders. (S,S)-TAK-418 also ameliorates ASD-like behaviors in rodent models affected by maternal exposure to valproate or poly I:C. (S,S)-TAK-418 modulates gene expression differently across various models and ages, indicating its potential as a therapeutic agent for conditions like autism spectrum disorder and schizophrenia.
    (S,S)-TAK-418
  • HY-144673
    LSD1-IN-12
    		Inhibitor
    LSD1-IN-12 (compound 2) is a potent LSD1 inhibitor, with Ki values of 1.1 μM (LSD1), 61 μM (LSD2), 2.3 μM (MAO-A), and 3.5 μM (MAO-B), respectively.
    LSD1-IN-12
  • HY-173135
    PROTAC KDM4 degrader-1
    		Degrader
    PROTAC KDM4 degrader-1 (Compound 11) is a KDM4-targeted proteolysis targeting chimeras (PROTAC) degrader. PROTAC KDM4 degrader-1 can degrade KDM4A-C while sparing KDM4D. PROTAC KDM4 degrader-1 exhibits potent antiproliferative activity in esophageal cancer cells. PROTAC KDM4 degrader-1 induces apoptosis and cell cycle arrest, and inhibits histone H3 lysine demethylation. (Blue: E3 ligase ligand (HY-112078), Black: linker (HY-W013381); Pink: ligand for target protein (HY-173136) ).
    PROTAC KDM4 degrader-1
  • HY-145861
    LSD1-IN-14
    		Inhibitor
    LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells.
    LSD1-IN-14
  • HY-144675
    LSD1-IN-13
    		Inhibitor
    LSD1-IN-13 (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 induces differentiation of AML (acute myeloid leukemia) cell lines.
    LSD1-IN-13
  • HY-B0546AS
    Procaine-d4 hydrochloride
    Procaine-d4 (hydrochloride) is the deuterium labeled Procaine hydrochloride. 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-d<sub>4</sub> hydrochloride
  • HY-146285
    LSD1-IN-20
    		Inhibitor
    LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively.
    LSD1-IN-20
  • HY-143238
    FY-56
    		Inhibitor
    FY-56 is a highly potent and selective LSD1/KDM1A inhibitor (IC50=42 nM) and exhibits high selectivity over MAO-A/B. FY-56 induces differentiation of MOLM-13 and MV4-11 cell and has the potential for AML research.
    FY-56
  • HY-173123
    LSD1-IN-40
    		Inhibitor
    LSD1-IN-40 (Compound 9e) is a potent LSD1 inhibitor, with an IC50 of 9.85 nM. LSD1-IN-40 exhibits exceptional selectivity for LSD1 over both MAOs and hERG. LSD1-IN-40 exhibits significant inhibitory activity against leukemia cells (MV-4-11, HL-60, and THP-1 cells). LSD1-IN-40 can induce apoptosis in MV-4-11 cells. LSD1-IN-40 has the potential for the research of acute myeloid leukemia.
    LSD1-IN-40
  • HY-151192
    LSD1/2-IN-3
    		Inhibitor
    LSD1/2-IN-3 is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a Ki value of 11 nM instead of 7 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, LSD1/2-IN-1 inhibits LSD1 cell proliferation.
    LSD1/2-IN-3
  • HY-139600
    KDM2B-IN-3
    		Inhibitor
    KDM2B-IN-3 is a histone demethylase KDM2B inhibitor extracted from patent WO2016112284A1, compound 183c. KDM2B-IN-3 can be used for the research of cancer.
    KDM2B-IN-3
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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