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Results for "

demethylases

" in MedChemExpress (MCE) Product Catalog:

236

Inhibitors & Agonists

4

Screening Libraries

19

Peptides

15

Natural
Products

12

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15648B
    GSK-J4
    Maximum Cited Publications
    55 Publications Verification

    Histone Demethylase Apoptosis Cancer
    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 .
    GSK-J4
  • HY-127103
    FB23-2
    25+ Cited Publications

    Apoptosis Cancer
    FB23-2 is a potent and selective inhibitor of mRNA N 6-methyladenosine (m 6A) demethylase FTO, with an IC50 of 2.6 μM. FB23-2 has anti-proliferation activity. FB23-2 can be used for the research of acute myeloid leukemia (AML) .
    FB23-2
  • HY-13643
    Daminozide
    3 Publications Verification

    Environmental Pollutants Histone Demethylase Cancer
    Daminozide, a plant growth regulator, is a selective inhibitor of the human KDM2/7 histone demethylases, with IC50s of 0.55, 1.5 and 2.1 μM for PHF8, KDM2A, and KIAA1718, respectively. Daminozide has >100-fold selectivity for KDM2/7 subfamily versus other demethylase subfamily members tested .
    Daminozide
  • HY-134124

    Reactive Oxygen Species (ROS) Metabolic Disease
    Glutathione ethyl ester is a cell-permeable GSH donor and provides an efficient supply of GSH to the oocyte. Glutathione ethyl ester shows positive effect on the in vitro production of embryos by enhancement of the antioxidative defense .
    Glutathione ethyl ester
  • HY-137187
    FB23
    2 Publications Verification

    Fat Mass and Obesity-associated Protein (FTO) Cancer
    FB23 is a potent and selective FTO demethylase inhibitor with an IC50 of 60 nM. FB23 directly binds to FTO and selectively inhibits FTO's mRNA N 6-methyladenosine (m6A) demethylase activity .
    FB23
  • HY-15648F
    GSK-J4 hydrochloride
    Maximum Cited Publications
    55 Publications Verification

    Histone Demethylase Cancer
    GSK-J4 hydrochloride 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 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1 .
    GSK-J4 hydrochloride
  • HY-112623
    Vafidemstat
    2 Publications Verification

    ORY-2001

    Histone Demethylase Monoamine Oxidase Neurological Disease
    Vafidemstat (ORY-2001) is an oral, brain penetrant, dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor .
    Vafidemstat
  • HY-12635
    SP2509
    10+ Cited Publications

    Histone Demethylase Apoptosis Cancer
    SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with an IC50 of 13 nM .
    SP2509
  • HY-15648
    GSK-J1
    15+ Cited Publications

    Histone Demethylase Cancer
    GSK-J1, a chemical probe, is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
    GSK-J1
  • HY-129388B
    Pulrodemstat benzenesulfonate
    4 Publications Verification

    CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate

    Histone Demethylase Inflammation/Immunology Cancer
    Pulrodemstat (CC-90011) benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat benzenesulfonate is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
    Pulrodemstat benzenesulfonate
  • HY-12782T
    Iadademstat dihydrochloride
    5+ Cited Publications

    ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride

    Histone Demethylase Cancer
    Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
    Iadademstat dihydrochloride
  • HY-18632
    GSK2879552
    15+ Cited Publications

    Histone Demethylase Cancer
    GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity .
    GSK2879552
  • HY-109169
    Bomedemstat
    3 Publications Verification

    IMG-7289

    Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
    Bomedemstat
  • HY-B0735A
    Fenoldopam mesylate
    4 Publications Verification

    Fenoldopam methanesulfonate; SKF-82526 mesylate

    Dopamine Receptor Apoptosis Cardiovascular Disease Cancer
    Fenoldopam mesylate (SKF-82526) is a D1 receptor agonist and a novel lysine-specific demethylase 1 (LSD1) inhibitor (IC50=0.8974 μM). Fenoldopam mesylate shows anti-hypertensive effects, anti-cancer cell proliferation activity and can induce cells apoptosis .
    Fenoldopam mesylate
  • HY-100546A
    GSK-LSD1 dihydrochloride
    10+ Cited Publications

    Histone Demethylase Monoamine Oxidase Cancer
    GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.
    GSK-LSD1 dihydrochloride
  • HY-12725
    ML324
    5+ Cited Publications

    Histone Demethylase HSV CMV Cancer
    ML324 is a potent JMJD2 demethylase inhibitor with antiviral activity. ML324 also exhibits inhibition for the histone demethylase KDM4B, with an IC50 of 4.9 μM. ML324 has potent anti-viral activity against both herpes simplex virus (HSV) and human cytomegalovirus (hCMV) infection via inhibition viral IE gene expression .
    ML324
  • HY-W015114

    (S)-2-Hydroxyglutaric acid disodium

    Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite Cancer
    L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively .
    L-2-Hydroxyglutaric acid disodium
  • HY-111048
    Corin
    5 Publications Verification

    Histone Demethylase HDAC Cancer
    Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.
    Corin
  • HY-18632A
    GSK2879552 dihydrochloride
    15+ Cited Publications

    Histone Demethylase Cancer
    GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity .
    GSK2879552 dihydrochloride
  • HY-139348
    PFI-90
    1 Publications Verification

    Histone Demethylase Apoptosis Cancer
    PFI-90 is a selective inhibitor of histone demethylase (KDM3B) that inhibits PAX3-FOXO1 action. PFI-90 induces apoptosis and myogenic differentiation, resulting in the cell death increased. PFI-90 has the potential for the antitumor activity. (patent WO2021101929A1).
    PFI-90
  • HY-W017132

    MOFs Histone Demethylase Cancer
    2,4-PDCA (2,4 pyridine dicarboxylic acid) is a broad-spectrum inhibitor of 2OG oxygenase, including JmjC domain-containing family of histone demethylases (JHDMs). 2,4-PDCA is a target chemical in the field of bio-based plastics .
    2,4-PDCA
  • HY-19612A
    DDP-38003 dihydrochloride
    1 Publications Verification

    Histone Demethylase Cancer
    DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM .
    DDP-38003 dihydrochloride
  • HY-113039

    (S)-2-Hydroxyglutaric acid

    Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite Cancer
    L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively .
    L-2-Hydroxyglutaric acid
  • HY-139434

    Histone Demethylase Cancer
    JMJD6-IN-1 is a JMJD6 inhibitor, with an inhibition rate of 82% at 10 μM. JMJD6-IN-1 inhibits MCF-7 and HCC4006 cell proliferation with IC50 values of 19.2 μM and 25.2 μM. JMJD6-IN-1 inhibits JMJD6 demethylase activity. JMJD6-IN-1 can be used for the research of lung adenocarcinoma, prostate cancer, breast cancer, pancreatic cancer, colon cancer, oral squamous cell carcinoma, and glioblastoma .
    JMJD6-IN-1
  • HY-15648A
    GSK-J2
    4 Publications Verification

    Histone Demethylase Cancer
    GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A.
    GSK-J2
  • HY-A0278

    (-)-Hexaconazol

    Environmental Pollutants Reactive Oxygen Species (ROS) Fungal SOD Infection Endocrinology
    Hexaconazole is a demethylation enzyme inhibitor and a synthetic fungicide that targets many fungi, especially ascomycetes and basidiomycetes, and it can enhance the activity of SOD and peroxidase. Hexaconazole causes endocrine disorders in zebrafish larvae .
    Hexaconazole
  • HY-P1108A
    Astressin 2B TFA
    1 Publications Verification

    CRFR Neurological Disease Inflammation/Immunology
    Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .
    Astressin 2B TFA
  • HY-P1108
    Astressin 2B
    1 Publications Verification

    CRFR Neurological Disease Inflammation/Immunology
    Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .
    Astressin 2B
  • HY-N2560

    Senecionan-11,16-dione, 12-hydroxy-; Aureine; Senecionin

    Others Metabolic Disease
    Senecionine (Senecionan-11,16-dione, 12-hydroxy-) is a pyrrolizidine alkaloid could be isolated from Senecio vulgaris. Senecionine decreases the activities of glutathione S-transferase, aminopyrine demethylase and arylhydrocarbon hydroxylase (AHH) .
    Senecionine
  • HY-141677

    Histone Demethylase Cancer
    INCB059872 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 can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 can be used for the research of myeloid leukemia .
    INCB059872
  • HY-109169A
    Bomedemstat ditosylate
    3 Publications Verification

    IMG-7289 ditosylate

    Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
    Bomedemstat ditosylate
  • HY-122635A

    Histone Demethylase Neurological Disease
    T-448 is a specific, orally active, CNS-penetrant and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons .
    T-448
  • HY-108706

    Histone Demethylase Cancer
    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 .
    KDM2A/7A-IN-1
  • HY-101928
    KDM4D-IN-1
    2 Publications Verification

    Histone Demethylase Cancer
    KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM.
    KDM4D-IN-1
  • HY-109169B
    Bomedemstat hydrochloride
    3 Publications Verification

    IMG-7289 hydrochloride

    Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
    Bomedemstat hydrochloride
  • HY-103085
    T-3775440 hydrochloride
    3 Publications Verification

    Histone Demethylase Cancer
    T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM.
    T-3775440 hydrochloride
  • HY-110277

    Histone Demethylase Cancer
    S2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s .
    S2101
  • HY-179610

    Histone Demethylase Cancer
    YU185530 is a JARID1 histone demethylase inhibitor .
    YU185530
  • HY-W173146

    DNA/RNA Synthesis Cancer
    ALKBH5-IN-4 (compound 3) is a RNA m6A demethylase ALKBH5 inhibitor with an IC50 of 0.84 μM. ALKBH5-IN-4 shows inhibitory effect on leukemia cells[1].
    ALKBH5-IN-4
  • HY-151106

    Fat Mass and Obesity-associated Protein (FTO) Cancer
    FTO-IN-8 (FTO-43) is a N6-methyladenosine demethylase (FTO) (fat mass- and obesity-associated protein) inhibitor with the IC50 value of 5.5 μM. FTO-IN-8 has anti-cancer cell proliferative activity .
    FTO-IN-8
  • HY-141677A

    Histone Demethylase Cancer
    INCB059872 dihydrochloride 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 dihydrochloride can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 dihydrochloride can be used for the research of myeloid leukemia .
    INCB059872 dihydrochloride
  • HY-112308
    NCGC00247743
    2 Publications Verification

    Histone Demethylase Cancer
    NCGC00247743 is a histone lysine demethylase KDM4 inhibitor.
    NCGC00247743
  • HY-15648D
    GSK-J1 lithium salt
    15+ Cited Publications

    Histone Demethylase Cancer
    GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
    GSK-J1 lithium salt
  • HY-129388A
    Pulrodemstat
    4 Publications Verification

    CC-90011; LSD1-IN-7

    Histone Demethylase Inflammation/Immunology Cancer
    Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
    Pulrodemstat
  • HY-109169C
    Bomedemstat dihydrochloride
    3 Publications Verification

    IMG-7289 dihydrochloride

    Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
    Bomedemstat dihydrochloride
  • HY-117426

    Fat Mass and Obesity-associated Protein (FTO) Cancer
    MO-I-500 is a pharmacological of FTO inhibitor with an IC50 of 8.7 μM for the inhibition of purified FTO demethylase catalyzing demethylation of an artificial small methylated substrate. MO-I-500 can be used for the research of rare panresistant triple-negative inflammatory breast cancer .
    MO-I-500
  • HY-125796

    Dopamine β-hydroxylase Neurological Disease
    U-14624 is a potent and orally active dopamine beta-hydroxylase inhibitor. U-14624 suppresses the activities of aminopyrine N-demethylase, aniline hydroxylase and p-nitroanisole O-demethylase enzymes .
    U-14624
  • HY-136522

    Histone Demethylase Apoptosis Cancer
    S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice .
    S2116
  • HY-117226A
    GSK 690 Hydrochloride
    3 Publications Verification

    Histone Demethylase Others
    GSK 690 (Hydrochloride) is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.
    GSK 690 Hydrochloride
  • HY-148807B

    (S)-QC8222 free base; (S)-TACH 101 free base

    Histone Demethylase Others
    (S)-Zavondemstat is the S-enantiomer of Zavondemstat (HY-148807). Zavondemstat is an inhibitor of histone lysine demethylase 4D (KDM4D) with antineoplastic activity [1] .
    (S)-Zavondemstat

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