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 (298)
Related Products (298)
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Antibodies (8)
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Histone Demethylase Isoform Comparison
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KDM1/CDK1-IN-1
0 ImagesCat. No.: HY-147901CAS No.: 2938990-92-0KDM1/CDK1-IN-1 (compound 4) is a potent KDM1 and CDK1 inhibitor, with IC50 values of 0.096 and 0.078 μM, respectively.KDM1/CDK1-IN-1 induces cell cycle arrest at G2/M phase and apoptosis in HOP-92 cells. KDM1/CDK1-IN-1 exhibits potent cytotoxic activity against the CCRF-CEM, HOP-92 and Hep-G2 cells, with IC50 values of 16.34, 3.45 and 7.79 μM, respectively.
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LSD1-IN-26
0 ImagesCat. No.: HY-149978CAS No.: 3041141-72-1LSD1-IN-26 (compound 12u) is a potent LSD1 inhibitor, with an IC50 of 25.3 nM. LSD1-IN-26 also inhibits MAO-A (IC50=1234.57 nM) and MAO-B (IC50=3819.27 nM). LSD1-IN-26 significantly induces apoptosis in MGC-803 cells. LSD1-IN-26 can be used for gastric cancer research.
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LSD1-IN-21
0 ImagesCat. No.: HY-147697LSD1-IN-21 (compound 5a) is a potent and BBB-penetrated LSD1 (Lysine specific demethylase-1) inhibitor, with an IC50 of 0.956 µM. LSD1-IN-21 significantly reduces the pro-inflammatory cytokine TNF-α. LSD1-IN-21 shows good anticancer and anti-inflammatory activity.
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LSD1-IN-48
0 ImagesCat. No.: HY-181781CAS No.: 3104325-26-7LSD1-IN-48 is a tranylcypromine-pyrimidine derivative and selective LSD1 inhibitor with a human IC50 of 7.87 nM. LSD1-IN-48 increases H3K4me1/2 histone methylation levels. LSD1-IN-48 induces apoptosis, upregulates CD86, downregulates SOX2 and CD44, inhibits proliferation in cancer cells. LSD1-IN-48 can be used for the research of acute myeloid leukemia.
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LSD1-IN-35
0 ImagesCat. No.: HY-168086CAS No.: 2992690-04-5LSD1-IN-35 (Compound Z-1) is a selective LSD1 Inhibitor (IC50: 108 nM). LSD1-IN-35 inhibits the demethylation on H3K4me1/2. LSD1-IN-35 is an immunomodulator. LSD1-IN-35 promotes response of gastric cancer cells to T-cell killing effect by decreasing PD-L1 expression and further attenuates the PD-1/PD-L1 interaction.
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Toxoflavin (Standard)
0 ImagesSynonyms: Xanthothricin (Standard); Toxoflavine (Standard); PKF-118-310 (Standard)Toxoflavin (Standard) is the analytical standard of Toxoflavin. This product is intended for research and analytical applications. Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor and antibiotic activity[1][2].
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LSD1-IN-50
0 ImagesCat. No.: HY-188077CAS No.: 1340824-39-6LSD1-IN-50 is a lysine-specific histone demethylase 1 (LSD1) inhibitor. LSD1-IN-50 inhibits the proliferation of Kasumi-1 leukemia cells and shows binding affinity to LSD-1. LSD1-IN-50 can be used for the study of cancer, particularly leukemia.
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KDM2/7-IN-2
0 ImagesCat. No.: HY-187178CAS No.: 1966932-74-0KDM2A/7-IN-1 is a lysine demethylase 2A (KDM2A) inhibitor with a human IC50 of 11 nM. KDM2A/7-IN-1 requires co-factor 2-oxoglutarate (2OG) for binding and occupies the H3K36me2 substrate pocket via a dimethylated lysine 36-mimicking group. KDM2A/7-IN-1 represses E2F-regulated genes, induces epithelial-mesenchymal transition, DNA repair, and mTOR pathways in specific cells, and selectively inhibits proliferation of ALT-positive cancer cell lines. KDM2A/7-IN-1 can be used for the research of ALT-positive cancers.
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LSD1-IN-18
0 ImagesCat. No.: HY-146283CAS No.: 2983011-61-4LSD1-IN-18 (compound 7) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.156 μM and KD of 0.075 μM, respectively. LSD1-IN-18 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.16 and 0.21 μM, respectively.
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α-Hydroxyglutaric acid disodium (Standard)
0 ImagesCat. No.: HY-113038ARCAS No.: 40951-21-1Synonyms: 2-Hydroxyglutarate disodium (Standard); 2-Hydroxyglutaric acid disodium (Standard); 2-Hydroxypentanedioic acid disodium (Standard)Ophiopogonin D (Standard) is the analytical standard of Ophiopogonin D. This product is intended for research and analytical applications. Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.
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N19-0881
0 ImagesCat. No.: HY-136682CAS No.: 1613410-75-5
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LSD1-IN-25
0 ImagesCat. No.: HY-149968CAS No.: 2911585-60-7
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LSD1-IN-46
0 ImagesCat. No.: HY-179339CAS No.: 2982716-97-0LSD1-IN-46 is a potent and orally active Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.082 μM. LSD1-IN-46 interrupts the β-catenin-mediated transcriptional program, thereby suppressing the stemness of gastric cancer cells. LSD1-IN-46 exhibits strong anti-tumor activity. LSD1-IN-46 can be used for the research of gastric cancer.
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LSD1-IN-33
0 ImagesCat. No.: HY-163859CAS No.: 3048029-42-8LSD1-IN-33 (7d), an orally active LSD1 inhibitor with an IC50 of 4.51 nM, alleviates Ang II-induced NRCFs activation in vitro and reducing pathological myocardial remodeling in TAC-induced cardiac remodeling and heart failure in vivo.
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LSD1-IN-22
0 ImagesCat. No.: HY-151191CAS No.: 2821068-05-5LSD1-IN-22 is a potent Lysine-specific demethylase 1 (LSD1) inhibitor with a Ki value of 98 nM. LSD1-IN-22 has anti-proliferative activity against certain cancer cells.
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EED-IN-4
0 ImagesCat. No.: HY-182365EED-IN-4 is an orally active, EZH2-selective immunomodulator and EED-H3K27me3 inhibitor (EED, IC50=28.21 nM) with anti-inflammatory activity. In mouse models, EED-IN-4 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-4 reduces the infiltration of immune cells into the central nervous system and effectively alleviates spinal cord inflammation. EED-IN-4 shows weak inhibitory activity against hERG channels and is non-mutagenic, with no obvious toxicity observed upon long-term oral administration. EED-IN-4 can be used for the research of multiple sclerosis.
