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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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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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
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Tranylcypromine hemisulfate (Standard)
0 ImagesSynonyms: SKF 385 hemisulfate (Standard)Tranylcypromine (hemisulfate) (Standard) is the analytical standard of Tranylcypromine (hemisulfate). This product is intended for research and analytical applications. Tranylcypromine (SKF 385) hemisulfate is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hemisulfate is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis. Tranylcypromine has antidepressant effects.
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YUKA1 (Standard)
0 ImagesCat. No.: HY-100764RCAS No.: 708991-09-7YUKA1 (Standard) is the analytical standard of YUKA1 (HY-100764). This product is intended for research and analytical applications. YUKA1 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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NCGC00244536 (Standard)
0 ImagesSynonyms: KDM4B Inhibitor B3 (Standard)NCGC00244536 (Standard) (KDM4B Inhibitor B3 (Standard)) is the analytical standard of NCGC00244536 (HY-101799). This product is intended for research and analytical applications. NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM.
