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-113039
    L-2-Hydroxyglutaric acid
    		Inhibitor
    L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid 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
  • 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-132198
    JMJD7-IN-1
    		Inhibitor 98.57%
    JMJD7-IN-1 is a potent JMJD7 inhibitor, with an IC50 of 6.62 μM. JMJD7-IN-1 shows good inhibitory activity against cells expressing a high level of JMJD7.
    JMJD7-IN-1
  • HY-123419
    CPI-4203
    		Inhibitor ≥99.0%
    CPI-4203 is a potent KDM5A inhibitor with an IC50 of 250 nM. CPI-4203 is competitive with 2-oxoglutarate (2-OG). CPI-4203 is structurally related to CPI-455 (HY-100421) but is less potent.
    CPI-4203
  • HY-149091
    KDM5B-IN-4
    		Inhibitor 99.68%
    KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC50 of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs.
    KDM5B-IN-4
  • HY-139560
    KDM2B-IN-1
    		99.19%
    KDM2B-IN-1 is a histone demethylase (kdm2b) inhibitor and can be used for hyperproliferative diseases research.
    KDM2B-IN-1
  • HY-162301
    P3FI-63
    		Inhibitor 98.35%
    P3FI-63 is a KDM3B inhibitor with a IC50 value of 7 μM. P3FI-63 has antitumor activity.
    P3FI-63
  • HY-19612B
    DDP-38003 trihydrochloride
    		Inhibitor
    DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
    DDP-38003 trihydrochloride
  • 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.
    Eicosapentaenoic Acid-d<sub>5</sub>
  • HY-100624
    Ryuvidine
    		99.40%
    Ryuvidine is a potent inhibitor of SET domain-containing protein 8(SETD8) with an IC50 of 0.5 µM and suppresses monomethylation of H4K20. Ryuvidine also inhibits CDK4 with an IC50 of 6.0 μM. Ryuvidine also inhibits KDM5A and blocks DNA synthesis. Ryuvidine has anticancer activity against tumors such as breast cancer. Ryuvidine improves arthritis.
    Ryuvidine
  • HY-W025799
    N-Benzylideneaniline
    		Inhibitor 99.97%
    N-Benzylideneaniline is an inhibitor of xylinostilbene-α,β-dioxygenase (LSD).
    N-Benzylideneaniline
  • 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-136522
    S2116
    		Inhibitor 98.15%
    S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice.
    S2116
  • HY-P2257
    H3K4(Me3) (1-20)
    		98.69%
    H3K4(Me3) (1-20) is a histone peptide. Trimethylation of histone H3 on lysine 4 (H3K4 me3) is found in active euchromatin but not in silent heterochromatin.
    H3K4(Me3) (1-20)
  • HY-158432
    GT-653
    		Degrader 99.84%
    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-121522
    SD-70
    		Inhibitor 99.20%
    SD-70 is an inhibitor for histone demethylase JMJD2C and exhibits antitumor efficacy. SD-70 inhibits viability of cancer cells CWR22Rv1 (9% cell survival at 10 μM), PC3 (14% cell survival at 2 μM) and DU145 (26% cell survival at 2 μM).
    SD-70
  • 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-121095
    Bizine
    		Inhibitor
    Bizine, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>Ki of 59 nM. Bizine can modulate bulk histone methylation in cancer cells. Bizine shows neuroprotective effects.
    Bizine
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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