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demethylases

" in MedChemExpress (MCE) Product Catalog:

137

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2

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8

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9

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6

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-137187

    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-116034

    Cytochrome P450 Bacterial Fungal Infection
    Arasertaconazole is a potent 14α-lanosterol demethylase inhibitor. Arasertaconazole has antifungal and antibacterial activity .
    Arasertaconazole
  • HY-122746

    Histone Methyltransferase Cancer
    E67-2, as the E67 derivative, is a low-toxicity, selective KIAA1718 Jumonji domain inhibitor with an IC50 value of 3.4 µM. E67-2 selectively inhibits histone H3 lysine 9 (H3K9) Jumonji demethylase as well as histone H3 lysine 4 (H3K4) demethylase .
    E67-2
  • HY-160183

    Histone Demethylase Cancer
    LSD1-IN-29 (compound 6) is a Lysine specific demethylase 1 (LSD1) inhibitor with the IC50 of 19 nM .
    LSD1-IN-29
  • HY-151194

    Histone Demethylase Cancer
    LSD1/2-IN-4, a PCPA derivative, is an inhibitor of lysine-specific demethylase 1 (LSD1) and lysine-specific demethylase 2 (LSD2). LSD1/2-IN-4 inhibits LSD1 and LSD2 with Ki values of 0.11 μM and 130 μM, respectively. LSD1/2-IN-4 can be used for the research of several cancers including T-cell acute lymphoblastic leukemia (TALL) .
    LSD1/2-IN-4
  • HY-141677

    Histone Demethylase Cancer
    INCB059872 is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 can be used for the research of myeloid leukemia .
    INCB059872
  • HY-141677A

    Histone Demethylase Cancer
    INCB059872 dihydrochloride is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 dihydrochloride can be used for the research of myeloid leukemia .
    INCB059872 dihydrochloride
  • 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-13643
    Daminozide
    2 Publications Verification

    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-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-117426

    Others 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-139348

    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-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-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-147697

    Histone Demethylase TNF Receptor Inflammation/Immunology Cancer
    LSD1-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 .
    LSD1-IN-21
  • HY-W017132

    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-15648F
    GSK-J4 hydrochloride
    Maximum Cited Publications
    34 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-127103
    FB23-2
    5+ 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-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-146670

    Histone Demethylase Cancer
    KDM5B-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 .
    KDM5B-IN-3
  • HY-15648B
    GSK-J4
    Maximum Cited Publications
    34 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-152032

    Histone Demethylase Cancer
    LSD1-IN-23 is a competitive/non-competitive mixed inhibitor of lysine specific demethylase 1 (LSD1). LSD1-IN-23 has LSD1 inhibitory activity with an IC50 value of 0.58 μM. LSD1-IN-23 can be used for the research of neuroblastoma (NB) .
    LSD1-IN-23
  • HY-109169

    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-109169B

    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-109169C

    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-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-109169A

    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-131970

    Histone Demethylase HDAC Cancer
    LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histone deacetylase 6 (HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM) .
    LSD1/HDAC6-IN-1
  • 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-<em>Demethylase</em>/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-<em>Demethylase</em>/DNA Gyrase-IN-1
  • HY-156405

    Fat Mass and Obesity-associated Protein (FTO) Autophagy Metabolic Disease
    FTO-IN-10 (compound 7) is a potent human demethylase FTO (the fat mass and obesity-associated protein) inhibitor with an IC50 of 4.5 μM. FTO-IN-10 enters the FTO’s structural domain II binding pocket through hydrophobic and hydrogen bonding interactions. FTO-IN-10 induces DNA damage and autophagic cell death in A549 cells .
    FTO-IN-10
  • HY-112308
    NCGC00247743
    1 Publications Verification

    Histone Demethylase Cancer
    NCGC00247743 is a histone lysine demethylase KDM4 inhibitor.
    NCGC00247743
  • HY-122635A

    Histone Demethylase Neurological Disease
    T-448 is a specific, orally active 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-15774A

    Histone Demethylase Cancer
    CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
    CBB1003 hydrochloride
  • HY-15774

    Histone Demethylase Cancer
    CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
    CBB1003
  • HY-122635

    Histone Demethylase Neurological Disease
    T-448 free base is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons .
    T-448 free base
  • 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-12635
    SP2509
    5+ 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
    5+ Cited Publications

    Histone Demethylase Cancer
    GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
    GSK-J1
  • HY-103085
    T-3775440 hydrochloride
    2 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-117226A
    GSK 690 Hydrochloride
    1 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-117226

    Histone Demethylase Cancer
    GSK 690 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
  • 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-15648D

    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-136523

    Histone Demethylase Apoptosis Cancer
    S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells .
    S2157
  • HY-100546A
    GSK-LSD1 dihydrochloride
    5 Publications Verification

    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-15648G

    Histone Demethylase Cancer
    GSK-J1 sodium is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 value of 60 nM towards KDM6B .
    GSK-J1 sodium
  • HY-148807

    QC8222 free base; TACH 101 free base

    Histone Demethylase Cancer
    Zavondemstat (QC8222; TACH 101) is an inhibitor of histone lysine demethylase 4D (KDM4D) with antineoplastic activity .
    Zavondemstat
  • 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-129388A

    CC-90011; LSD1-IN-7

    Histone Demethylase 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, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
    Pulrodemstat

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