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 (299)
Related Products (299)
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Antibodies (8)
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Histone Demethylase Isoform Comparison
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LSD1-IN-49
0 ImagesCat. No.: HY-186116CAS No.: 1422533-70-7LSD1-IN-49 is an irreversible LSD1/KDM1A inhibitor with an IC50 of 29 nM against hLSD1. LSD1-IN-49 irreversibly inhibits the enzymatic activity of LSD1 by forming an adduct with flavin adenine dinucleotide (FAD) in the binding pocket of LSD1. LSD1-IN-49 is applicable to research related to schizophrenia, autism spectrum disorder and Huntington's disease.
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YU185530
0 ImagesCat. No.: HY-179610CAS No.: 951971-87-2YU185530 is a JARID1 histone demethylase inhibitor.
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DDP-38003
0 ImagesCat. No.: HY-19612CAS No.: 1831167-97-5DDP-38003 (Compound 15) is an orally active KDM1A/LSD1 inhibitor with an IC50 value of 84 nM. DDP-38003 exhibits anticancer activity against promyelocytic leukemia.
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LSD1-UM-109
0 ImagesCat. No.: HY-149595CAS No.: 2252446-26-5LSD1-UM-109 is a ighly potent and reversible LSD1 inhibitor with an IC50 of 3.1 nM. LSD1-UM-109 inhibits cell growth with IC50 values of 0.6 nM in the MV4;11 acute leukemia cell line and 1.1 nM in the H1417 small-cell lung cancer cell line.
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JHDM-IN-1
0 ImagesJHDM-IN-1 (Compound 1) is a Jumonji C domain-containing HDMs (JHDM) inhibitor with IC50s of 3.4, 4.3, 5.9, 10 and 43 μM against JMJD2C, JMJD2A, JMJD2E, PHF8 and JMJD3, respectively.
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LSD1-IN-41
0 ImagesCat. No.: HY-172519CAS No.: 2295907-44-5
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TAK-418 free base
0 ImagesCat. No.: HY-138830BCAS No.: 1818252-52-6TAK-418 free base is an orally active, blood-brain barrier-penetrant LSD1 inhibitor with a human IC50 of 2.9 nM. TAK-418 free base irreversibly inhibits LSD1 by forming a compact flavin-FAD adduct with the catalytic domain FAD, blocking the demethylation of H3K4me1/2 and H3K9me1/2 without disrupting the LSD1-GFI1B interaction. TAK-418 free base restores normally dysregulated brain gene expression and DNA methylation, increases H3K4me1/2/3 and H3K9me2 at the Ucp2 locus, and induces Ucp2 mRNA expression. TAK-418 free base rescues defective H3K4 histone modifications, normalizes adult neurogenesis, and improves recognition memory, social behavior, and cognition in rodent models. TAK-418 free base can be used in research related to neurodevelopmental disorders, Alzheimer's disease, and autism spectrum disorders.
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LSD1-IN-38
0 ImagesCat. No.: HY-170403LSD1-IN-38 (Compound 23e) is a reversible, orally active inhibitor for lysine specific demethylase 1 (LSD1) with an IC50 of 1.2 nM. LSD1-IN-38 inhibits the proliferation of cancer cells MV4-11, Kasumi-1 and NCI-H526, with IC50 of 5, 4 and 11 nM, respectively. LSD1-IN-38 activates CD86 expression with an EC50 of 0.034 μM, and induces differentiation in MV4−11 cell. LSD1-IN-38 exhibits antitumor efficacy in mouse models.
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INCB059872 TFA
0 ImagesCat. No.: HY-141677CCAS No.: 1802909-50-7INCB059872 TFA is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor that achieves inhibitory activity through the formation of covalent FAD-adducts. INCB059872 TFA can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 TFA can be used for the research of myeloid leukemia.
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S9-CMC1 TFA
0 ImagesCat. No.: HY-P10819S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models.
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KDM4C-IN-2
0 ImagesCat. No.: HY-116796CAS No.: 23705-85-3
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INCB059872 tosylate
0 ImagesCat. No.: HY-141677BCAS No.: 2081940-67-0INCB059872 tosylate is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor that achieves inhibitory activity through the formation of covalent FAD-adducts. INCB059872 tosylate can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 tosylate can be used for the research of myeloid leukemia.
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(1R,2S)-NCD38 TFA
0 ImagesCat. No.: HY-112304ACAS No.: 2078047-42-2(1R,2S)-NCD38 TFA is an enantiomer of NCD38 TFA. NCD38 TFA is a LSD1-selective inhibitor.
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S1427
0 ImagesCat. No.: HY-146380CAS No.: 2447061-40-5S1427 is a tranylcypromine-derived LSD1 inhibitor with the IC50 of 390 nM and Ki of 80 nM. S1427 exhibits desirable hERG channel inhibition and microsomal stability profiles. Inhibition of LSD1 partially reduces the proliferation of cancer cells.
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GSK 690
0 ImagesCat. No.: HY-117226CAS No.: 2101305-84-2GSK 690 is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.
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LSD1-IN-23
0 ImagesCat. No.: HY-152032CAS No.: 3033660-66-8LSD1-IN-23 is a competitive/non-competitive mixed inhibitor of lysine specific demethylase 1 (LSD1). LSD1-IN-23 has LSD1 inhibitory activity with an IC50 value of 0.58 μM. LSD1-IN-23 can be used for the research of neuroblastoma (NB).
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LSD1/2-IN-4
0 ImagesCat. No.: HY-151194CAS No.: 2821068-09-9LSD1/2-IN-4, a PCPA derivative, is an inhibitor of lysine-specific demethylase 1 (LSD1) and lysine-specific demethylase 2 (LSD2). LSD1/2-IN-4 inhibits LSD1 and LSD2 with Ki values of 0.11 μM and 130 μM, respectively. LSD1/2-IN-4 can be used for the research of several cancers including T-cell acute lymphoblastic leukemia (TALL).
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NCL1
0 ImagesCat. No.: HY-12645CAS No.: 1196119-03-5NCL1 is a phenylcyclopropylamine (PCPA)-based Lysine-specific demethylase 1 (LSD1) inhibitor. NCL1 selectively inhibits LSD1 in preference to LSD2, with IC50 values of 2.5 and 26 μM for LSD1 and LSD2, respectively.
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NCD38 TFA
0 ImagesCat. No.: HY-112304CAS No.: 1456907-40-6NCD38 TFA is a LSD1-selective inhibitor.
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cis-4-Br-2,5-F2-PCPA
0 ImagesCat. No.: HY-151190CAS No.: 2821068-03-3Synonyms: S1024cis-4-Br-2,5-F2-PCPA (S1024) is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a Ki value of 94 nM instead of 8.4 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, cis-4-Br-2,5-F2-PCPA inhibits LSD1 cell proliferation and by increasing the level of dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells.
