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-148807A
    Zavondemstat L-lysine
    		Inhibitor
    Zavondemstat (QC8222; TACH 101) (L-lysine) is an inhibitor of histone lysine demethylase 4D (KDM4D) with antineoplastic activity.
    Zavondemstat L-lysine
  • HY-129388A
    Pulrodemstat
    		Inhibitor
    Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
    Pulrodemstat
  • HY-109169
    Bomedemstat
    		Inhibitor 99.55%
    Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.
    Bomedemstat
  • 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.
    KDM4-IN-2
  • HY-102047
    KDOAM-25
    		Inhibitor
    KDOAM-25 is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.
    KDOAM-25
  • HY-136523
    S2157
    		Inhibitor 98.44%
    S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.
    S2157
  • HY-W015114R
    L-2-Hydroxyglutaric acid (disodium) (Standard)
    		Inhibitor
    L-2-Hydroxyglutaric acid (disodium) (Standard) is the analytical standard of L-2-Hydroxyglutaric acid (disodium). This product is intended for research and analytical applications. 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 (disodium) (Standard)
  • HY-P2255
    H3K4(Me) (1-20)
    		99.82%
    H3K4(Me) (1-20), a histone peptide. H3K4me is an intricately regulated posttranslational modification, which is broadly associated with enhancers and promoters of actively transcribed genomic loci.
    H3K4(Me) (1-20)
  • HY-120766
    NCDM-32B
    		Inhibitor
    NCDM-32B is a potent and selective KDM4 inhibitor that impaires viability and transforming phenotypes of breast cancer.
    NCDM-32B
  • HY-161470
    WS-384
    		Inhibitor 98.23%
    WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC).
    WS-384
  • HY-128912
    Arborinine
    		Inhibitor 99.87%
    Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity .
    Arborinine
  • HY-149249
    MY-943
    		Inhibitor 98.01%
    MY-943 is a potent tubulin polymerization and LSD1 inhibitor with anticancer activity. MY-943 induces G2/M phase arrest and apoptosis, and inhibits cell migration. MY-943 can be used for gastric cancer research.
    MY-943
  • HY-112308
    NCGC00247743
    		Inhibitor 98.61%
    NCGC00247743 is a histone lysine demethylase KDM4 inhibitor.
    NCGC00247743
  • HY-113038AS1
    α-Hydroxyglutaric acid-d4 disodium
    α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium[1]. 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[2].
    α-Hydroxyglutaric acid-d<sub>4</sub> disodium
  • HY-15313B
    CBB1007 hydrochloride
    		Inhibitor ≥98.0%
    CBB1007 Hcl is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.
    CBB1007 hydrochloride
  • HY-15313C
    CBB1007 trihydrochloride
    		Inhibitor
    CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.
    CBB1007 trihydrochloride
  • HY-B0660R
    Eicosapentaenoic Acid (Standard)
    		Activator
    Eicosapentaenoic Acid (Standard) is the analytical standard of Eicosapentaenoic Acid. This product is intended for research and analytical applications. 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.
    Eicosapentaenoic Acid (Standard)
  • HY-15648D
    GSK-J1 lithium salt
    		Inhibitor 98.26%
    GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
    GSK-J1 lithium salt
  • HY-15313
    CBB1007
    		Inhibitor
    CBB1007 is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
    CBB1007
  • HY-100859
    LSD1-IN-5
    		Inhibitor
    LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
    LSD1-IN-5
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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