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 Controls
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Histone Demethylase Ligands
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Histone Demethylase Related Products (297)
Related Products (297)
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Antibodies (8)
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Histone Demethylase Isoform Comparison
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DC551040
0 ImagesCat. No.: HY-183105CAS No.: 2133291-32-2DC551040 is an orally active and selective lysine demethylase 1 (LSD1) inhibitor with a human IC50 of 2.14 nM. DC551040 binds to LSD1 via π-π stacking with Trp552, polar interactions with Phe538, and covalent adduct formation with FAD, and disrupts the LSD1-GFI1B-CoREST complex. DC551040 induces H3K4me2 accumulation, apoptosis, and cell differentiation, activates STAT5, NF-κB, AKT, and IL6-STAT3 pathways, and upregulates IL6 expression. DC551040 can be used for the research of acute myeloid leukemia.
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LSD1-IN-16
0 ImagesCat. No.: HY-144757CAS No.: 3033060-68-0LSD1-IN-16 (compound 4b) is a potent LSD1 inhibitor. LSD1-IN-16 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.015, 0.024, and 0.366 μM, respectively. LSD1-IN-16 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 15.2 μM.
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(2R)-Octyl-α-hydroxyglutarate (Standard)
0 ImagesSynonyms: (2R)-Octyl-2-HG (Standard)(2R)-Octyl-α-hydroxyglutarate (Standard) is the analytical standard of (2R)-Octyl-α-hydroxyglutarate. This product is intended for research and analytical applications. (2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) is a modified form of D-isomer 2-Hydroxyglutarate.
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Pulrodemstat hydrochloride
0 ImagesCat. No.: HY-129388CCAS No.: 1821307-11-2Synonyms: CC-90011 hydrochloride; LSD1-IN-7 hydrochloridePulrodemstat (CC-90011) hydrochloride is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 value of 0.25 nM. Pulrodemstat hydrochloride is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat hydrochloride induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
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Tranylcypromine-d5 hydrochloride
0 ImagesCat. No.: HY-17447SACAS No.: 107077-98-5Synonyms: SKF 385-d5 hydrochlorideTranylcypromine-d5 (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis.
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GSK-J1 sodium
0 ImagesCat. No.: HY-15648GCAS No.: 1797832-71-3GSK-J1 sodium is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 value of 60 nM towards KDM6B.
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AW4
0 ImagesCat. No.: HY-173590CAS No.: 2455469-18-6AW4 is a LSD1 inhibitor. AW4 inhibits LSD1 ΔTTAS activity in H3K4me2 demethylation assays. AW4 can be used for research of drug resistance.
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L-2-Hydroxyglutaric acid-d5 disodium
0 ImagesCat. No.: HY-W744986Synonyms: (2S)-2-Hydroxyglutaric acid-d5 disodiumL-2-Hydroxyglutaric acid-d5 disodium ((2S)-2-Hydroxyglutaric acid-d5 disodium) is the deuterium labeled L-2-Hydroxyglutaric acid disodium (HY-W015114). 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.
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JQKD82
0 ImagesCat. No.: HY-138691CAS No.: 2410512-38-6Synonyms: JADA82; PCK82JQKD82 (JADA82) is a cell-permeable and selective KDM5 inhibitor. JQKD82 increases H3K4me3 and can be used for the research of multiple myeloma.
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Eicosapentaenoic acid 1,2,3,4,5-13C5
0 ImagesCat. No.: HY-B0660S1Purity: 99.9%Synonyms: EPA 1,2,3,4,5-13C, FA 20:5-13C5Eicosapentaenoic acid 1,2,3,4,5-13C5 (EPA 1,2,3,4,5-13C, FA 20:5-13C5) is 13C labeled Eicosapentaenoic Acid. 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.
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CBB1003 hydrochloride
0 ImagesCat. No.: HY-15774ACAS No.: 2070015-02-8CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
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GSK-J4 (Standard)
0 ImagesGSK-J4 (Standard) is the analytical standard of GSK-J4. This product is intended for research and analytical applications. GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.
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KdM2A/7A-IN-1 (Standard)
0 ImagesCat. No.: HY-108706RCAS No.: 2169272-46-0KdM2A/7A-IN-1 (Standard) is the analytical standard of KdM2A/7A-IN-1 (HY-108706). This product is intended for research and analytical applications. KdM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KdM2A/7A, with an IC50 of 0.16 μM for KdM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases.
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KDM4D-IN-1 (Standard)
0 ImagesCat. No.: HY-101928RCAS No.: 2098902-68-0KDM4D-IN-1 (Standard) is the analytical standard of KDM4D-IN-1 (HY-101928). This product is intended for research and analytical applications. KDM4D-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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S2101 (Standard)
0 ImagesCat. No.: HY-110277RCAS No.: 1239262-36-2
