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MGMT inhibitor

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-W002585
    O6-Benzylguanine
    2 Publications Verification

    DNA/RNA Synthesis Apoptosis Cancer
    O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity .
    O6-Benzylguanine
  • HY-13668
    Lomeguatrib
    Maximum Cited Publications
    6 Publications Verification

    PaTrin-2

    DNA Methyltransferase Cancer
    Lomeguatrib is a O 6-methylguanine-DNA methyltransferase (MGMT) inhibitor, with IC50s of 9 nM in cell-free assay and ~6?nM in MCF-7 cells.
    Lomeguatrib
  • HY-13057
    O6BTG-octylglucoside
    3 Publications Verification

    Glucose-conjugated MGMT inhibitor

    DNA Methyltransferase Cancer
    O6BTG-octylglucoside is a potent O 6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells.
    O6BTG-octylglucoside
  • HY-119390

    DNA Methyltransferase Cancer
    AA-CW236 is a MGMT (O6-methylguanine DNA methyltransferase) inhibitor. AA-CW236 targets MGMT active site Cys145 for covalent modification .
    AA-CW236
  • HY-W002585R

    Reference Standards DNA/RNA Synthesis Apoptosis Cancer
    O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity .
    O6-Benzylguanine (Standard)
  • HY-146651

    Glutathione Peroxidase Cardiovascular Disease Inflammation/Immunology
    MPO-IN-4 (compound 12) is a potent and selective myeloperoxidase (MPO) inhibitor with an IC500 of 25 nM. MPO-IN-4 has no effect on methyl guanine methyl transferase (MGMT) .
    MPO-IN-4
  • HY-175299

    Hedgehog Apoptosis DNA Methyltransferase Cancer
    Hedgehog IN-11 is an orally active Hedgehog inhibitor. Hedgehog IN-11 downregulates the expression of O6-methylguanine-DNA methyltransferase (MGMT) to impair the Temozolomide (TMZ) (HY-17364) resistance by inhibiting the Hedgehog pathway. Hedgehog IN-11 shows improved inhibition of cell migration and invasion, and induced cell apoptosis in TMZ-resistant GBM cell lines. Hedgehog IN-11 is predicted by computer simulation to have good blood-brain barrier penetration. Hedgehog IN-11 can be used for the study of glioblastoma (GBM) .
    Hedgehog IN-11
  • HY-13786

    DNA Methyltransferase Cancer
    O6BTG-C8-αGlu is an O6-methylguanine-DNA methyltransferase (MGMT) inhibitor with an IC50 of 0.45 μM. At a concentration of 0.1 μM, O6BTG-C8-αGlu can completely inhibit MGMT in HeLaS3 cells. Even when applied chronically at high doses (up to 20 μM), it does not exhibit cytotoxicity. O6BTG-C8-αGlu is suitable for research on MGMT-related cancer diseases .
    O6BTG-C8-αGlu
  • HY-169002

    Phosphatase Cancer
    PP5-IN-2 is an orally active and selective protein phosphatase 5 (PP5) inhibitor with an IC50 value of 0.9 μM. PP5-IN-2 activates p53 and downregulates cyclin D1 and MGMT, which shows potency in cell cycle arrest and reverses Temozolomide (TMZ) (HY-17364) resistance in the U87 MG cell line. PP5-IN-2 effectively inhibits tumor growth in the xenograft mouse model .
    PP5-IN-2
  • HY-180540

    DNA Methyltransferase Neurological Disease Cancer
    MGMT-IN-1 (Compound 2) is a light-activated MGMT inhibitor. MGMT-IN-1 can effectively enhance the cytotoxicity of Temozolomide (TMZ) (HY-17364) only under light conditions, significantly increasing the DNA damage caused by TMZ. MGMT-IN-1 can be used for the study of chordoma .
    MGMT-IN-1
  • HY-138195

    DNA/RNA Synthesis Apoptosis FAK Src MMP Autophagy Cancer
    NEO212 is an orally active, blood-brain barrier permeable conjugate of Temozolomide (TMZ) (HY-17364) and Perillyl Alcohol (POH) (HY-N7000), with potent anticancer activity. NEO212 overcomes classical TMZ resistance and DNA alkylation by depleting MGMT. By inhibiting the FAK/Src signaling pathway, NEO212 reduces the production of MMP2 and MMP9, induces mesenchymal-epithelial transition, and inhibits the migration, invasion and tumor progression of glioma stem cells. NEO212 disrupts autophagy flux to enhance mitochondrial apoptosis; it induces differentiation of acute myeloid leukemia (AML) cells into macrophages and proliferation arrest .
    NEO212

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