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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KDM5B-IN-3
0 ImagesCat. No.: HY-146670CAS No.: 1385101-10-9KDM5B-IN-3 (Compound 5) is a histone lysine specific demethylase 5B (KDM5B/JARID1B) inhibitor with an IC50 of 9.32 μM. KDM5B-IN-3 can be used for the research of gastric cancer.
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LSD1-IN-19
0 ImagesCat. No.: HY-146284CAS No.: 2983011-81-8LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.108 μM and KD of 0.068 μM, respectively. LSD1-IN-19 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.17 and 0.40 μM, respectively.
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LSD1-IN-42
0 ImagesCat. No.: HY-172809LSD1-IN-42 (Compound 7ae) is an orally active LSD1 inhibitor that potently inhibits LSD1 activity (IC50 = 0.08 μM). LSD1-IN-42 downregulates PD-L1 expression and enhances T cell-mediated tumor killing effects. LSD1-IN-42 demonstrates significant anti-gastric cancer activity by inhibiting tumor cell invasion and migration.
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CBN209350
0 ImagesCat. No.: HY-126207CAS No.: 726201-10-1CBN209350 is a selective KDM4 inhibitor with an IC50 of 4 μM. CBN209350 exerts antiproliferative effects on prostate cancer cells. CBN209350 can be used for the research of prostate cancer.
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(S,S)-TAK-418
0 ImagesCat. No.: HY-138830ACAS No.: 1818253-48-3(S,S)-TAK-418 is a potent inhibitor of lysine-specific demethylase 1 (LSD1), demonstrating significant normalization of aberrant gene expression in neurodevelopmental disorders. (S,S)-TAK-418 also ameliorates ASD-like behaviors in rodent models affected by maternal exposure to valproate or poly I:C. (S,S)-TAK-418 modulates gene expression differently across various models and ages, indicating its potential as a therapeutic agent for conditions like autism spectrum disorder and schizophrenia.
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Zavondemstat sodium
0 ImagesCat. No.: HY-148807CCAS No.: 2908753-07-9Synonyms: QC8222 sodium; TACH 101 sodiumZavondemstat (QC8222; TACH 101) sodium is an orally active pan-KDM4 inhibitor, with a IC50 ≤ 0.08 μM against human KDM4A-D and a Kᵢ of 0.52 μM against human KDM4C. Zavondemstat sodium induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat sodium suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat sodium can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer.
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LSD1-IN-12
0 ImagesCat. No.: HY-144673CAS No.: 1228143-76-7
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LSD1-IN-14
0 ImagesCat. No.: HY-145861CAS No.: 2698340-11-1LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells.
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LSD1-IN-13
0 ImagesCat. No.: HY-144675CAS No.: 2170212-33-4LSD1-IN-13 (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 induces differentiation of AML (acute myeloid leukemia) cell lines.
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LSD1-IN-20
0 ImagesCat. No.: HY-146285CAS No.: 1239589-91-3LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively.
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LSD1-IN-10
0 ImagesCat. No.: HY-136878CAS No.: 1235864-15-9LSD1-IN-10 is a LSD1/MAO inhibitor with LSD1 IC50 of 5 nM, MAO-A IC50 of 16 μM, and MAO-B IC50 of 7.4 μM. LSD1-IN-10 suppresses enzymatic activity of LSD1, MAO-A, and MAO-B. LSD1-IN-10 can be used for the research of cancer, alzheimer's disease, parkinson's disease, huntington's disease.
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LSD1-IN-40
0 ImagesCat. No.: HY-173123LSD1-IN-40 (Compound 9e) is a potent LSD1 inhibitor, with an IC50 of 9.85 nM. LSD1-IN-40 exhibits exceptional selectivity for LSD1 over both MAOs and hERG. LSD1-IN-40 exhibits significant inhibitory activity against leukemia cells (MV-4-11, HL-60, and THP-1 cells). LSD1-IN-40 can induce apoptosis in MV-4-11 cells. LSD1-IN-40 has the potential for the research of acute myeloid leukemia.
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LSD1/2-IN-3
0 ImagesCat. No.: HY-151192CAS No.: 2821068-07-7LSD1/2-IN-3 is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a Ki value of 11 nM instead of 7 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, LSD1/2-IN-1 inhibits LSD1 cell proliferation.
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KDM2B-IN-3
0 ImagesCat. No.: HY-139600CAS No.: 1966933-87-8KDM2B-IN-3 is a histone demethylase KDM2B inhibitor extracted from patent WO2016112284A1, compound 183c. KDM2B-IN-3 can be used for the research of cancer.
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TPC-144
0 ImagesCat. No.: HY-123577CAS No.: 2098621-17-9TPC-144 is a LSD1/KDM1A inhibitor. TPC-144 inhibits LSD1, and leads to a decrease in the protein level of DNMT1, causing low methylation of the LINE-1 element. TPC-144 can also produce a synergistic effect with Decitabine (HY-A0004) (a DNMT inhibitor), jointly promoting DNA demethylation and thereby inducing differentiation and apoptosis of leukemia cells. TPC-144 has also demonstrated anti-tumor efficacy in acute myeloid leukemia (AML) models. TPC-144 can be used for the study of AML.
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LSD1-IN-49 hydrochloride
0 ImagesCat. No.: HY-186116ACAS No.: 1422534-06-2LSD1-IN-49 hydrochloride (Compound (±) 1) is an irreversible LSD1/KDM1A inhibitor with an IC50 of 29 nM against hLSD1. LSD1-IN-49 hydrochloride 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 hydrochloride is applicable to research related to schizophrenia, autism spectrum disorder and Huntington's disease.
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LSD1-IN-51
0 ImagesCat. No.: HY-187092CAS No.: 1423715-30-3LSD1-IN-51 is a selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 8.7 nM. LSD1-IN-51 selectively inhibits H3K4me1/2 demethylation by binding to the FAD domain of LSD1, while disrupting the interaction between LSD1 and multiprotein complexes such as HDAC1/2 and CoREST. LSD1-IN-51 can be used for cancer research.
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Tubulin/LSD1-IN-1
0 ImagesCat. No.: HY-176283Tubulin/LSD1-IN-1 is an effective dual inhibitor of Tubulin polymerization and LSD1 (IC50 = 1.72 μM). Tubulin/LSD1-IN-1 has broad-spectrum antiproliferative activity against cancer cell lines. Tubulin/LSD1-IN-1 inhibits tubulin polymerization by targeting colchicine binding sites, thereby disrupting the microtubule network in gastric cancer cells. Tubulin/LSD1-IN-1 increases the methylation levels of H3K4me1/2 and H3K9me2/3, thereby achieving epigenetic regulation. Tubulin/LSD1-IN-1 induces G2/M arrest, promotes apoptosis, and effectively inhibits colony formation of gastric cancer cells.
