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 Isoform Specific Products
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Histone Demethylase Inhibitors
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Histone Demethylase Antagonist
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Histone Demethylase Activators
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Histone Demethylase Degraders
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Histone Demethylase Ligands
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Histone Demethylase Related Products (298)
Related Products (298)
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Antibodies (8)
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Histone Demethylase Isoform Comparison
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KDM4D-IN-1
0 ImagesKDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM.
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Helenalin acetate
0 ImagesHelenalin acetate, a natural NF-κB inhibitor, is a potent C/EBPβ inhibitor. Helenalin acetate has anti-inflammatory and anticancer activities.
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KDM2B-IN-4
0 ImagesKDM2B-IN-4 (Compound 182b) is a histone demethylase KDM2B inhibitor with an IC50 of 1.12 nM. KDM2B-IN-4 can be used for the research of hyperproliferative diseases such as cancers.
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KDM5B-IN-4
0 ImagesKDM5B-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.
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PBIT
0 ImagesPBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1) histone demethylase with an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with IC50s of 6 μM and 4.9 μM, respectively.
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KDM4-IN-3
0 ImagesKDM4-IN-3 (Compound 15) is a KDM4 inhibitor (IC50 = 871 nM) that exhibits improved potency in biochemical assays. KDM4-IN-3 is cell-permeable and kills prostate cancer cells at low micro molar concentrations. KDM4-IN-3 inhibits growth of prostate cancer cell lines and increases the H3K9me3 abundance. KDM4-IN-3 can be studied in research for prostate cancer.
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T-448
0 ImagesT-448 is a specific, orally active, CNS-penetrant and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons.
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Bomedemstat dihydrochloride
0 ImagesCat. No.: HY-109169CPurity: 99.55%Synonyms: IMG-7289 dihydrochlorideBomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.
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L-2-Hydroxyglutaric acid
0 ImagesCat. No.: HY-113039CAS No.: 13095-48-2Synonyms: (S)-2-Hydroxyglutaric acidL-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.
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Arborinine
0 ImagesArborinine 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 .
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Pulrodemstat
0 ImagesSynonyms: CC-90011; LSD1-IN-7Pulrodemstat (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, MAO-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
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SD-70
0 ImagesSD-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).
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KDM2B-IN-1
0 ImagesKDM2B-IN-1 (example 32) is a histone demethylase (kdm2b) inhibitor with an IC50 of 0.016 nM. KDM2B-IN-1 can be used for hyperproliferative diseases research.
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P3FI-63
0 ImagesP3FI-63 is a KDM3B inhibitor with a IC50 value of 7 μM. P3FI-63 has antitumor activity.
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N-Benzylideneaniline
0 ImagesCat. No.: HY-W025799CAS No.: 538-51-2Synonyms: N-Benzalaniline; N-PhenylbenzylimineN-Benzylideneaniline is an inhibitor of xylinostilbene-α,β-dioxygenase (LSD).
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YUKA1
0 ImagesYUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM. YUKA1 has less inhibitory active on KDM5C (IC50 = 7.12 μM) and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 can increase H3K4me3 levels and inhibit cell proliferation. YUKA1 can be used for the research of cancer, such as lung and breast cancers.
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T-3775440 hydrochloride
0 ImagesT-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM.
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L-2-Hydroxyglutaric acid disodium (Standard)
0 ImagesCat. No.: HY-W015114RCAS No.: 63512-50-5Synonyms: (S)-2-Hydroxyglutaric acid disodium (Standard)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.
