2. Epigenetics
  3. Histone Demethylase

Histone Demethylase

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 Related Products (216):

Cat. No. Product Name Effect Purity
  • HY-15648B
    GSK-J4 Inhibitor
    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[1][2][3]. GSK-J4 induces endoplasmic reticulum stress-related apoptosis[4].
  • HY-100421
    CPI-455 Inhibitor 98.95%
    CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents[1].
  • HY-12304
    IOX1 Inhibitor 99.72%
    IOX1, 5-Carboxy-8-hydroxyquinoline, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC50 values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively[1][2]. IOX1 also inhibits ALKBH5[3].
  • HY-18632
    GSK2879552 Inhibitor 99.90%
    GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity[1][2].
  • HY-B0660
    Eicosapentaenoic Acid Activator
    Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation[1][2][3].
  • HY-168968S
    ZJY-54
    ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity[1].
  • HY-173136
    KDM4 ligand-1 Ligand
    KDM4 ligand-1 is a ligand for target protein (histone lysine demethylase KDM4) for PROTACs. KDM4 ligand-1 can be used in the synthesis of PROTACs (HY-173135)[1].
  • 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) )[1].
  • 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[1][2].
  • HY-144675A
    LSD1-IN-13 hydrochloride Inhibitor
    LSD1-IN-13 hydrochloride (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 hydrochloride can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 hydrochloride induces differentiation of AML (acute myeloid leukemia) cell lines[1].
  • HY-18632A
    GSK2879552 dihydrochloride Inhibitor 99.19%
    GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity[1][2].
  • HY-114519
    Helenalin acetate Inhibitor 98.59%
    Helenalin acetate, a natural NF-κB inhibitor, is a potent C/EBPβ inhibitor. Helenalin acetate has anti-inflammatory and anticancer activities[1].
  • HY-151483
    TK-129 Inhibitor
    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[1].
  • HY-B0660S
    Eicosapentaenoic Acid-d5 Activator 99.90%
    Eicosapentaenoic Acid-d5 is the deuterium labeled Eicosapentaenoic Acid. Eicosapentaenoic Acid (EPA; Timnodonic acid) is an omega-3 fatty acid.
  • HY-115747
    Namoline Inhibitor
    Namoline, a γ-pyrone, is a selective and reversible Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 51 μM in a HRP-coupled enzymatic assay. Namoline impairs LSD1 demethylase activity and blocks cell proliferation. Namoline has the potential for androgen-dependent prostate cancer research[1].
  • HY-144755
    MC2652 Inhibitor
    MC2652 (compound 1a) is a potent LSD1 inhibitor. MC2652 displays high inhibiting effects in MV4-11 and NB4 leukaemia cells. MC2652 shows antiproliferative activity against prostate cancer LNCaP cells[1].
  • HY-P2253
    H3K27(Me2) (15-34)
    H3K27(Me2) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me)[1][2].
  • HY-15648H
    GSK-J5 hydrochloride Inhibitor
    GSK-J5 hydrochloride is a cell-permeable?ester derivative of?GSK J2 (HY-15648A), inactive. GSK-J5 hydrochloride is also an?isomer of GSK-J4 (HY-15648B) and often used as a negative group[1].
  • HY-15774A
    CBB1003 hydrochloride Inhibitor
    CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
  • HY-128343
    KDM4-IN-2 Inhibitor 98.29%
    KDM4-IN-2 (Compound 19a) is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively[1].