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demethylase activity

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-127103
    FB23-2
    Maximum Cited Publications
    26 Publications Verification

    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-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-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-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-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-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-16012A
    Domatinostat
    3 Publications Verification

    4SC-202 free base

    HDAC Apoptosis Cancer
    Domatinostat (4SC-202 free base) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
    Domatinostat
  • 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-16012
    Domatinostat tosylate
    3 Publications Verification

    4SC-202

    HDAC Apoptosis Cancer
    Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
    Domatinostat tosylate
  • 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-15221
    Methylstat
    3 Publications Verification

    Apoptosis Histone Demethylase MDM-2/p53 Cardiovascular Disease Cancer
    Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis .
    Methylstat
  • 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-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-117766

    Fungal Cytochrome P450 Infection
    PC945, a potent, long-acting antifungal triazole, possesses activity against a broad range of both azole-susceptible and azole-resistant strains of Aspergillus fumigatus. PC945 is also a potent, tightly binding inhibitor of A. fumigatus sterol 14α-demethylase activity, CYP51A and CYP51B, with IC50s of 0.23 μM and 0.22 μM, respectively .
    PC945
  • 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-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-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-14282
    Lanoconazole
    1 Publications Verification

    Fungal Infection Inflammation/Immunology
    Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi?in vitro?and?in vivo . Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis .
    Lanoconazole
  • 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-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-156202

    Histone Demethylase PD-1/PD-L1 Apoptosis Cancer
    Geranylgeranoic acid (Compound 5) is inhibits lysine-specific demethylase 1 (LSD1) with an IC50 value of 46.97 µM. Geranylgeranoic acid induces apoptosis via loss of the mitochondrial membrane potential and activation of interleukin-1β-converting enzyme (ICE) and cysteine protease precursor 32 (CPP32) in Huh7 and PLC/PRF/5 human hepatoma cells and MLE-10 transformed mouse hepatocytes. Geranylgeranoic acid an isoprenoid with anticancer activity, which is found in S. chinensis .
    Geranylgeranoic acid
  • HY-117089

    Environmental Pollutants Fungal Infection
    Tetraconazole is a selective irreversible inhibitor of 14-α-sterol demethylase (CYP51) with antifungal activity. Tetraconazole competitively binds to the enzyme to block fungal ergosterol synthesis, resulting in cell membrane damage. The EC50 of tetraconazole against wheat pathogens is 0.382-0.802 mg/L, and the EC50 against onion root tip meristem cell growth is 6.7 mg/L, and (R)-(+)-Tetraconazole is 1.49-1.98 times more active than (S)-(-)-Tetraconazole. Tetraconazole can also induce oxidative stress and chromosomal aberrations in plant cells .
    Tetraconazole
  • 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-149145

    Anaplastic lymphoma kinase (ALK) Fat Mass and Obesity-associated Protein (FTO) Cancer
    Ena15 is an ALKBH5 inhibitor. Ena15 enhances the demethylase activity of FTO. Ena15 increases m 6A RNA level, and stabilizes FOXM1 mRNA. Ena15 suppresses the growth activity of glioblastoma multiforme .
    Ena15
  • 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-169131

    AMPK Cancer
    ALKBH1-IN-4 prodrug (Compound 29E) is a prodrug of a DNA N6-methyladenine demethylase ALKBH1 inhibitor that significantly increases the abundance of 6mA in cells and upregulates the AMPK signaling pathway, thereby inhibiting the viability of gastric cancer cells. ALKBH1-IN-4 prodrug exhibits excellent cellular activity and favorable metabolic exposure in vivo, and holds promise for research in gastric cancer .
    ALKBH1-IN-3 prodrug
  • 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-W1127089

    Fungal Cytochrome P450 Interleukin Related Infection Inflammation/Immunology
    Antifungal agent 136 (Compound M-15) is an irreversible fungal lanosterol 14α-demethylase (CYP51) inhibitor. Antifungal agent 136 exhibits potent antifungal activity against drug-resistant Candida albicans and downregulates IL-6 expression. Antifungal agent 136 is promising for research of fungal infection and inflammatory disease .
    Antifungal agent 136
  • HY-15313C
    CBB1007 trihydrochloride
    2 Publications Verification

    Histone Demethylase Metabolic Disease Cancer
    CBB1007 trihydrochloride is a reversible and selective LSD1 inhibitor with an IC50 of 5.27 µM for human LSD1. CBB1007 trihydrochloride significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 trihydrochloride shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 trihydrochloride is studied in non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma .
    CBB1007 trihydrochloride
  • HY-W015114R

    (S)-2-Hydroxyglutaric acid disodium (Standard)

    Reference Standards Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite Cancer
    L-2-Hydroxyglutaric acid (disodium) (Standard) is the analytical standard of L-2-Hydroxyglutaric acid (disodium). This product is intended for research and analytical applications. 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 (Standard)
  • 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-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
  • HY-14282A

    Fungal Infection Inflammation/Immunology
    (Z)-Lanoconazole is the Z configuration of Lanoconazole. Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo . Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis .
    (Z)-Lanoconazole
  • HY-129388C

    CC-90011 hydrochloride; LSD1-IN-7 hydrochloride

    Histone Demethylase Inflammation/Immunology Cancer
    Pulrodemstat (CC-90011) hydrochloride is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 value of 0.25 nM. Pulrodemstat hydrochloride is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat hydrochloride induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
    Pulrodemstat hydrochloride
  • HY-N10340

    Clauszoline I

    Others Cancer
    Clausine E, is a alkaloid which can be isolated from Clausena excavata, is a inhibitor of fat mass and obesity-associated protein (FTO) demethylase. Clausine E shows inhibitory activities against proliferation of synoviocytes and cancer cells.
    Clausine E
  • HY-178162

    Fungal Cytochrome P450 Infection
    CYP51-IN-27 is a sterol 14α-demethylase CYP51 inhibitor with an IC50 of 0.3434 μg/mL. CYP51-IN-27 exhibits antifungal activity and inhibits the production of fungal ergosterol. CYP51-IN-27 can be used for the research of infection, such as rice sheath blight .
    CYP51-IN-27
  • HY-105191

    RS-21607

    Cytochrome P450 Reactive Oxygen Species (ROS) Metabolic Disease
    Azalanstat (RS-21607) is an inhibitor of heme oxygenase and lanosterol 14α-demethylase, with inhibitory activity against HO-1 (IC50 = 5.5 µM) and HO-2 (IC50 = 24.5 µM). Azalanstat reduces the maturation rate of rat oocytes, increases rat oocyte degeneration, and partially inhibits progesterone production in preovulatory follicles of rats .
    Azalanstat
  • HY-179339

    Histone Demethylase Cancer
    LSD1-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 .
    LSD1-IN-46
  • HY-W264454

    Bacterial Infection
    Antibacterial agent 303 (compound 3) is an antibacterial agent exhibiting potent antibacterial activity against MDR strains, with MICs of 10 and 100 µg/mL against Pseudomonas aeruginosa MDR1 and Staphylococcus aureus MDR strains, respectively. Antibacterial agent 303 displays strong binding affinities to E. coli DNA gyrase and Candida albicans lanosterol 14α-demethylase. Antibacterial agent 303 can be used for drug-resistant infections research .
    Antibacterial agent 303
  • HY-117219

    Cytochrome P450 HMG-CoA Reductase (HMGCR) Endogenous Metabolite Metabolic Disease
    SKF 104976 is a 3,2-carboxylic acid derivative with potent 14-alpha-demethylase (14 alpha DM) inhibitory activity. SKF 104976 inhibited 14 alpha DM activity by 50% at 2 nM in Hep G2 cell extracts. SKF 104976 inhibited the incorporation of [14C]acetate into cholesterol in intact cells at similar concentrations, accompanied by accumulation of lanosterol, and resulted in a 40-70% decrease in 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) activity. SKF 104976 did not affect the uptake and degradation of low-density lipoprotein in Hep G2 cells, indicating that HMGR and low-density lipoprotein receptor activities are not coordinately regulated under these conditions. The inhibitory effect of SKF 104976 on HMGR activity remained unchanged even when the flux of carbon units in the sterol synthesis pathway was reduced by 80%. SKF 104976 did not inhibit HMGR activity under conditions where sterol synthesis was almost completely blocked by lovastatin .
    SKF 104976
  • HY-B0735AR

    Fenoldopam methanesulfonate (Standard); SKF-82526 mesylate (Standard)

    Reference Standards Dopamine Receptor Apoptosis Cardiovascular Disease Cancer
    Fenoldopam (mesylate) (Standard) is the analytical standard of Fenoldopam (mesylate). This product is intended for research and analytical applications. 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 (Standard)
  • HY-147777

    Bacterial DNA/RNA Synthesis Infection
    14α-Demethylase/DNA Gyrase-IN-2 (Compound 6a) is a potent inhibitor of 14α-Demethylase/DNA Gyrase. 14α-Demethylase/DNA Gyrase-IN-2 has antimicrobial activities .
    14α-Demethylase/DNA Gyrase-IN-2
  • HY-147778

    Bacterial DNA/RNA Synthesis Infection
    14α-Demethylase/DNA Gyrase-IN-1 (Compound 7c) is a potent inhibitor of 14α-Demethylase/DNA Gyrase. 14α-Demethylase/DNA Gyrase-IN-1 has antimicrobial activities .
    14α-Demethylase/DNA Gyrase-IN-1
  • HY-116034

    Cytochrome P450 Bacterial Fungal Infection
    Arasertaconazole is a potent 14α-lanosterol demethylase inhibitor. Arasertaconazole has antifungal and antibacterial activity .
    Arasertaconazole
  • HY-115747

    Histone Demethylase Cancer
    Namoline, a γ-pyrone, is a selective and reversible Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 51 μM in a HRP-coupled enzymatic assay. Namoline impairs LSD1 demethylase activity and blocks cell proliferation. Namoline has the potential for androgen-dependent prostate cancer research .
    Namoline
  • HY-117869

    Antibiotic Fungal Infection
    AFK-108 is a potent antifungal agent. AFK-108 inhibits the activity of 14 alpha-demethylase .
    AFK-108
  • HY-168527

    Histone Demethylase Cancer
    Acaricide agent 1 (Compound 7l) is a potent LSD1 inhibitor. LSD1 exhibits excellent acaricidal activity against egg of T. cinnabarinus with a LC50 of 0.0035 mg/L .
    Acaricide agent 1

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