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Histone Demethylase

Histone demethylase proteins have a variety of domains that serve different functions. These functions include binding to the histone (or sometimes the DNA on the nucleosome), recognizing the correct methylated amino acid substrate and catalyzing the reaction, and binding cofactors. Cofactors include: alpha-keto glutarate (JmjC-domain containing demethylases), CoREST (LSD), FAD, Fe (II) or NOG (N-oxalylglycine).

  • 3-pyridine toxoflavin
    T6773832502-20-8
    3-pyridine toxoflavin is a potent KDM4C inhibitor, IC50=19nM.
    • $195
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  • LSD1-IN-20
    T631401239589-91-3In house
    Lsd1-in-20 is a potent dual inhibitor of LSD1/G9a with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 showed antiproliferative activity against THP-1 leukemia cells and MDA-MB-231 breast cancer cells in vitro, with IC50 of 0.51 and 1.60 μM, respectively, at 72 h.
    • $397
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  • 5-Hydroxy-7-acetoxy-8-methoxyflavone
    TN312095480-80-1
    5-Hydroxy-7-acetoxy-8-methoxyflavone is a flavonoid compound that inhibits lipid peroxidation and may have anti-influenza virus activity.
    • $248
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  • Acetyl Pentapeptide-1 acetate
    T38318L
    Acetyl Pentapeptide-1 acetate is an histone deacetylase inhibitor.
    • $148
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  • KDM5-C49 HCl
    T27723L
    KDM5-C49 HCl (KDOAM-20 hydrochloride) is a potent and selective inhibitor of KDM5 demethylase. KDM5-C49 HCL(1596348-16-1 Free base) is a candidate compound for the treatment of cancer.
    • $195
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  • LSD1-IN-27
    T776352904571-94-2
    LSD1-IN-27 is a potent LSD1 inhibitor with an IC50 value of 13 nM.LSD1-IN-27 inhibited the stemness and migration of gastric cancer cells.LSD1-IN-27 inhibited the expression of PD-L1 in BGC-823 and MFC cells.LSD1-IN-27 potentiated the T-cell immune response against gastric cancer.
    • $158
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  • GSK2879552 2HCl (1401966-69-5(free base))
    T4418
    GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
    • $54
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    TargetMol | Citations Cited
  • Corin
    T108641808113-09-8In house
    Corin is an irreversible inhibitor of HDAC1(IC50 = 147 nM) and LSD1(Ki = 110 nM).
    • $179
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  • DDP-38003 dihydrochloride
    T10983L1831167-98-6In house
    DDP-38003 dihydrochloride is an orally available histone lysine-specific demethylase 1A (KDM1A/LSD1) inhibitor (IC50: 84 nM).
    • $73
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  • KDM4-IN-4
    T603542230475-63-3In house
    KDM4-IN-4 is a selective histone lysyl demethylase 4 (KDM4) inhibitor with anticancer activity, inhibits the KDM4A-Tudor structural domain, and inhibits intracellular binding of H3K4Me3 to the Tudor structural domain.KDM4-IN-4 is used in the study of cancer, obesity, and cardiovascular disease.
    • $293
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  • Zavondemstat
    T701211851412-93-5In house
    Zavondemstat (QC8222 free base) is a histone lysine demethylase 4 (KDM4) inhibitor with anticancer and antitumor activity for the study of triple-negative and breast cancers.
    • $152
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  • GSK-J4
    T31001373423-53-0In house
    GSK-J4 (GSK J4 HCl) is a potent H3K27me3 demethylase inhibitor, with IC50s of 8.6 μM and 6.6 μM towards KDM6B and KDM6A respectively. It is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.
    • $51
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  • KDM2A/7A-IN-1
    T117482169272-46-0In house
    KDM2A/7A-IN-1 is a cell-permeable and selective inhibitor of the histone lysine demethylase KDM2A/7A with potential antitumor activity for the study of duodenal adenomas and ossifying fibromucoid tumors.
    • $272 TargetMol
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  • QC6352
    T167001851373-36-8In house
    QC6352 is a selective and effective KDM4C inhibitor (IC50: 35 nM).
    • $1,520
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  • T-448
    T130571597426-53-3In house
    T-448 is an orally available and potent lysine-specific demethylase 1 inhibitor (IC50: 22 nM) that improves learning function in mice.T-448 can be used to study memory deficits.
    • $786
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  • TAK-418
    T392521818252-53-7In house
    TAK-418 is a selective and orally active inhibitor of LSD1 KDM1A enzyme with an IC50 of 2.9 nM. TAK-418 unlocks abnormal epigenetic mechanisms and improves autism symptoms in models of neurodevelopmental disorders.
    • $233
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  • Bomedemstat ditosylate
    T700081990504-72-7In house
    Bomedemstat ditosylate (IMG-7289 ditosylate) is an orally active lysine-specific demethylase 1 (LSD1) inhibitor with antitumor activity that potentiates the response to PD-1 inhibition in a homozygous model of SCLC, inhibits cancer cell proliferation, and induces apoptosis. Bomedemstat ditosylate can be used to study myeloproliferative neoplasms and myelofibrosis.
    • $117
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  • KDM5-C70
    T156481596348-32-1
    KDM5-C70 is an ethyl ester derivative of KDM5-C49. KDM5-C70 is an effective, cell-permeable, and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, inducing a genome-wide elevation of H3K4me3 levels.
    • $37
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    TargetMol | Citations Cited
  • IOX1
    T65455852-78-8
    IOX1 is the most effective broad-spectrum 2OG oxygenases(including the JmjC demethylases) inhibitor. The IC50 of IOX1 for KDM4A, KDM3A, is 0.6 and 0.1 uM, respectively.
    • $38
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  • AS8351
    T4100796-42-9
    AS8351 (NSC51355) is a histone demethylase inhibitor. It has been used in combination with CHIR99021, A 83-01, BIX01294, SC-1, Y-27632, OAC2, SU 16f, and JNJ-10198409 to induce reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.
    • $43
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  • ORY1001
    T69221431326-61-2
    ORY1001 (ORY 1001) is an orally active and selective lysine-specific demethylase LSD1 KDM1A inhibitor, with high selectivity against related FAD dependent aminoxidases with IC50 of <20 nM.
    • $54
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  • CPI-455
    T35521628208-23-0
    CPI-455 is a specific KDM5 inhibitor.
    • $37
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  • P3FI-63
    T84287931596-95-1
    P3FI-63 is a selective KDM3B inhibitor (IC50: 7 μM) with antitumor activity for the study of fusion-positive rhabdomyosarcoma and other transcriptionally addictive cancers.
    • $30
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  • LSD1-IN-30
    T839661289575-45-6
    LSD1-IN-30 is a lysine-specific demethylase 1 (LSD1) inhibitor with anticancer activity for the study of small cell lung cancer and acute myeloid leukemia.
    • $118
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  • JQKD82
    T399892410512-38-6
    JQKD82 is a selective inhibitor of KDM5 and increases H3K4me3. JQKD82 can be used in studies about the treatment of multiple myeloma.
    • $137
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  • FY-21
    T77583
    FY-21 is a selective LSD1 inhibitor (IC50= 340 nM) that inhibits proliferation and colony formation of leukemia cells, decreases mRNA levels of the transcription factors HOXA9 and MEIS1, and can be used in the study of leukemia.
    • $195
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  • GSK-690
    T274882101305-84-2
    GSK-690 is a selective and potent inhibitor of lysine demethylase 1 (LSD 1), which induces differentiation of leukemic stem cells in acute myeloid leukemia (AML), and can be used in the study of leukemias.
    • $293
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  • SD49-7
    T6778154009-54-0
    SD49-7 is an inhibitor of histone lysine demethylase 4 (KDM4) with an IC50 of 0.19 µM.
    • $55
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  • NCD38 TFA
    T78577
    NCD38 TFA serves as a selective inhibitor of LSD1 [1] [2].
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  • KDM5-IN-1
    T156491628210-26-3
    KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM.
    • $58
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  • LSD1-IN-25
    T748552911585-60-7
    LSD1-IN-25 (Compound 9j) is a potent, selective, and orally active inhibitor of LSD1, exhibiting an IC50 of 46 nM (Ki = 30.3 nM) and capable of inducing apoptosis in cancer cells [1].
    • Inquiry Price
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  • L-2-Hydroxyglutaric acid disodium
    T1374863512-50-5
    L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium) is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity(Km and Ki of 2.52 mM and 11.13 mM, respectively).
    • $45
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  • Daminozide
    T37191596-84-5
    Daminozide (Succinic Acid) is a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.
    • $42
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  • KDM4D-IN-1
    T42142098902-68-0
    KDM4D-IN-1 is a KDM4D inhibitor (IC50: 0.41±0.03 μM).
    • $70
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  • GSK-LSD1
    T822541431368-48-7
    GSK-LSD1, an LSD1 inhibitor, decreases food consumption and body weight while enhancing insulin sensitivity and glycemic regulation in murine obesity models. Additionally, it mitigates non-alcoholic fatty liver disease (NAFLD) and suppresses cytokine release induced by SARS-CoV-2 in COVID-19 peripheral blood mononuclear cells (PBMCs). Furthermore, GSK-LSD1 inhibits the proliferation and spread of cancer [1] [2] [3].
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  • RN-1 dihydrochloride
    T216521781835-13-9
    RN-1 dihydrochloride is an effective and selective irreversible inhibitor of lysine-specific demethylase 1 (LSD1, IC50 = 70 nM).
    • $42
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  • Tranylcypromine hemisulfate
    T794213492-01-8
    Tranylcypromine hemisulfate (Tranylcypromine Sulfate) is an inhibitor of monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1) with a rapid onset of activity.
    • $48
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  • GSK-J4 Hydrochloride
    T43831797983-09-5
    GSK-J4 Hydrochloride (GSK J4 HCl) is a cell permeable, potent and selective histone demethylase(JMJD3 )inhibitor. is an ethyl ester derivative of the GSK-J1 with an IC50 value greater than 50 μM in vitro.
    • $34
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  • Seclidemstat
    T45271423715-37-0
    Seclidemstat (SP-2577) is an effective LSD1 inhibitor, with a mean IC50 of 127 nM.
    • $41
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  • GSK467
    T54841628332-52-4
    GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).
    • $74
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  • KF 13218
    T11755127654-03-9
    KF 13218 is a selective, potent and long lasting thromboxane B2 (TXB2) synthase inhibitor with an IC50 value of 5.3±1.3 nM.
    • $1,520
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  • Procaine
    T002959-46-1
    Procaine (Vitamin H3) is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block.
    • $46
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  • GSK-J1 lithium salt
    T114752309668-29-7
    GSK-J1 lithium salt is an effective inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with an IC 50 of 60 nM for KDM6B.
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  • T-448 free base
    T130561597426-52-2
    T-448 free base is a specific, orally active and irreversible lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) inhibitor(IC50 of 22 nM).
    • $1,820
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  • Iadademstat dihydrochloride
    T58251431303-72-8
    Iadademstat dihydrochloride (ORY-1001(trans)) , a Potent and Selective Covalent KDM1A/LSD1 Inhibitor, for the Treatment of Acute Leukemia.
    • $38
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  • T-3775440 hydrochloride
    T130551422535-52-1
    T-3775440 hydrochloride is an irreversible inhibitor of lysine-specific histone demethylase (LSD1)(IC50 : 2.1 nM).
    • $97
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  • CPI-455 HCl
    T222992095432-28-1
    CPI-455 is a specific KDM5 inhibitor with IC50 value of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with target
    • $1,520
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  • Pulrodemstat benzenesulfonate
    T118822097523-60-7
    Pulrodemstat benzenesulfonate (CC-90011 benzenesulfonate) is a potent and orally active inhibitor of lysine specific demethylase-1 (LSD1) with anticancer activity.
    • $55
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  • GSK-LSD1 dihydrochloride
    T23152102933-95-7
    GSK-LSD1 dihydrochloride (GSK-LSD1 2HCl) is a specificity irreversible LSD1 inhibitor (IC50: 16 nM). The selectivity of GSK-LSD1 for LSD1 is >1000 fold over other closely related FAD utilizing enzymes (i.e. MAO-A, LSD2, MAO-B).
    • $34
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  • SP2509
    T23041423715-09-6
    SP2509 is a specific histone demethylase LSD1 inhibitor(IC50 =13 nM).
    • $52
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