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-164099
    LSD1/HDAC6-IN-2
    		Inhibitor 99.66%
    LSD1/HDAC6-IN-2 (JBI-802) is an orally active LSD1/HDAC6/MAO-A inhibitor, with IC50 values of 5 nM, 11 nM, and 5 nM, respectively. LSD1/HDAC6-IN-2 can inhibit the growth of multiple myeloma cells MM.1S, MM.1R, and RPMI-8226. LSD1/HDAC6-IN-2 can be used for research on diseases such as acute myeloid leukemia and lymphoma.
    LSD1/HDAC6-IN-2
  • HY-123194
    SIRT2/6-IN-1
    		98.44%
    SIRT2/6-IN-1 (Compound 5) is a SIRT6/SIRT2 inhibitor, with IC50s of 106 μM and 114 μM. SIRT2/6-IN-1 increases H3K9 acetylation, increases glucose uptake and reduces TNF-α secretion in cells.
    SIRT2/6-IN-1
  • 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-145259
    HDAC6-IN-3
    		Inhibitor ≥98.0%
    HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor. HDAC6-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    HDAC6-IN-3
  • HY-113038AS
    α-Hydroxyglutaric acid-13C5 disodium
    		99.80%
    α-Hydroxyglutaric acid-13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium 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-<sup>13</sup>C<sub>5</sub> disodium
  • HY-160191
    LSD1-IN-30
    		Inhibitor 99.03%
    LSD1-IN-30 (compound 3) is a potent inhibitor of lysine-specific demethylase 1 (LSD1), with the IC50 value of 0.291 μM.
    LSD1-IN-30
  • 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-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-141677
    INCB059872
    		Inhibitor 98.06%
    INCB059872 is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 can be used for the research of myeloid leukemia.
    INCB059872
  • 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-B0660S
    Eicosapentaenoic Acid-d5
    		Activator 99.00%
    Eicosapentaenoic Acid-d5 is the deuterium labeled Eicosapentaenoic Acid. Eicosapentaenoic Acid (EPA; Timnodonic acid) is an omega-3 fatty acid.
    Eicosapentaenoic Acid-d<sub>5</sub>
  • 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-158432
    GT-653
    		Degrader
    GT-653 is a PROTAC degrader for lysine-specific demethylase 5B (KDM5B). GT-653 degrades 68.35% KDM5B at 10 μM in a ubiquitin proteasome-dependent manner, upregulates H3K4me3 levels, and activates the type-I interferon signaling pathway in prostate cancer cells 22RV1. (Pink: KDM5B ligand (HY-158433); Black: Linker (HY-W004896); Blue: E3 ligase ligand (HY-103596))
    GT-653
  • HY-161470
    WS-384
    		Inhibitor
    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-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
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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