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-113038AR
    α-Hydroxyglutaric acid disodium (Standard)
    		Inhibitor
    Ophiopogonin D (Standard) is the analytical standard of Ophiopogonin D. This product is intended for research and analytical applications. Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.
    α-Hydroxyglutaric acid disodium (Standard)
  • HY-136682
    N19-0881
    		Inhibitor
    N19-0881 (Compound 33) is an orally active, potent and selective KDM5A/5B histone lysine demethylase inhibitor (IC50= 0.013 μM and 0.002 μM, respectively). N19-0881 is promising for research of epigenetically dysregulated tumors (e.g., breast cancer).
    N19-0881
  • HY-119617
    2-(3-Hydroxypicolinamido)acetic acid
    		Inhibitor
    2-(3-Hydroxypicolinamido)acetic acid is a 2OG oxygenase inhibitor with an IC50 value of 3.4 μM. 2-(3-Hydroxypicolinamido)acetic acid can be used as a functional probe for potential therapeutic research.
    2-(3-Hydroxypicolinamido)acetic acid
  • HY-149968
    LSD1-IN-25
    		Inhibitor
    LSD1-IN-25 (Compound 9j) is a potent, selective and orally active LSD1 inhibitor with an IC50 of 46 nM (Ki = 30.3 nM). LSD1-IN-25 induces cancer cell apoptosis.
    LSD1-IN-25
  • HY-17447B
    (1S,2R)-Tranylcypromine hydrochloride
    		Inhibitor
    (1S,2R)-Tranylcypromine ((1S,2R)-SKF 385) hydrochloride is a potent antidepressant agent. (1S,2R)-Tranylcypromine hydrochloride can inhibits MAO and LSD1.
    (1S,2R)-Tranylcypromine hydrochloride
  • HY-121095A
    Bizine dihydrochloride
    		Inhibitor 99.90%
    Bizine dihydrochloride, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>Ki of 59 nM. Bizine dihydrochloride can modulate bulk histone methylation in cancer cells. Bizine dihydrochloride shows neuroprotective effects.
    Bizine dihydrochloride
  • HY-175036
    YTHu78
    		Degrader
    YTHu78 is a KDM5B PROTAC-type degrader. YTHu78 induces KDM5B degradation via the ubiquitin-proteasome system and triggers apoptosis in MV-4-11 and MM.1S cell lines. YTHu78 exhibits significant antiproliferative activity against a variety of hematological cancer cell lines and can be used to study hematological cancers. (Pink: KDM5B ligand: (HY-116761); Blue: Thalidomide ligand: (HY-14658), Black + Pink: KDM5B ligand + linker: (HY-175145)).
    YTHu78
  • HY-179339
    LSD1-IN-46
    		Inhibitor
    LSD1-IN-46 is a potent and orally active Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.082 μM. LSD1-IN-46 interrupts the β-catenin-mediated transcriptional program, thereby suppressing the stemness of gastric cancer cells. LSD1-IN-46 exhibits strong anti-tumor activity. LSD1-IN-46 can be used for the research of gastric cancer.
    LSD1-IN-46
  • HY-183067
    TAS1440
    		Inhibitor
    TAS1440 is an orally active LSD1/KDM1A inhibitor with a human IC50 of 4.8 nM. TAS1440 non-covalently binds to the histone H3-binding pocket of LSD1, inhibiting demethylase activity and disrupting repressive complexes with INSM1 and SMAD2. TAS1440 activates tumor-suppressive TGF-β and NOTCH signaling pathways via transcriptional reprogramming. TAS1440 can be used for the research of small cell lung cancer, specifically the SCLC-A subtype.
    TAS1440
  • HY-163859
    LSD1-IN-33
    		Inhibitor
    LSD1-IN-33 (7d), an orally active LSD1 inhibitor with an IC50 of 4.51 nM, alleviates Ang II-induced NRCFs activation in vitro and reducing pathological myocardial remodeling in TAC-induced cardiac remodeling and heart failure in vivo.
    LSD1-IN-33
  • 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-182365
    EED-IN-4
    		Inhibitor
    EED-IN-4 is an orally active, EZH2-selective immunomodulator and EED-H3K27me3 inhibitor (EED, IC50=28.21 nM) with anti-inflammatory activity. In mouse models, EED-IN-4 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-4 reduces the infiltration of immune cells into the central nervous system and effectively alleviates spinal cord inflammation. EED-IN-4 shows weak inhibitory activity against hERG channels and is non-mutagenic, with no obvious toxicity observed upon long-term oral administration. EED-IN-4 can be used for the research of multiple sclerosis.
    EED-IN-4
  • 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-182891
    MC4455
    MC4455 is a LSD1/PRMT5 dual inhibitor. MC4455 inhibits the LSD1/CoREST and PRMT5/MEP50 complex with IC50 values of 0.104 μM and 0.014 μM. MC4455 covalently binds to LSD1’s FAD cofactor, stabilizes the LSD1/CoREST complex. MC4455 induces myeloid differentiation, alters transcriptomic profiles, drives alternative splicing changes, and impairs leukemic cell viability in AML cells. MC4455 can be used for the research of acute myeloid leukemia.
    MC4455
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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