2. Signaling Pathways
  3. Epigenetics
  4. DNA Methyltransferase
  5. MGMT Isoform

MGMT

MGMT encodes O6-methylguanine-DNA methyltransferase, also called AGT, a DNA repair protein that removes alkyl groups from O6-alkylguanine adducts[1]. Mechanistically, MGMT repairs cytotoxic O6-methylguanine and O6-chloroethylguanine lesions induced by methylating or chloroethylating agents, thereby limiting DNA damage signaling and alkylating-drug cytotoxicity[2][3]. In glioma, MGMT promoter methylation silences MGMT expression and predicts clinical response to alkylating agents, including temozolomide[4][5]. Compared with separate isoform targets, the retrieved literature describes MGMT/AGT as the same repair protein, so isoform-specific claims require additional evidence[1]. For experimental applications, O6-benzylguanine and O6-(4-bromothenyl)guanine have been used to inactivate MGMT, but normal-tissue MGMT inhibition can increase alkylating-drug toxicity[6].

MGMT Related Products (4):

Cat. No. Product Name Effect Purity
  • HY-13668
    Lomeguatrib
    		Inhibitor 99.77%
    Lomeguatrib is a O6-methylguanine-DNA methyltransferase (MGMT) inhibitor, with IC50s of 9 nM in cell-free assay and ～6?nM in MCF-7 cells.
  • HY-13057
    O6BTG-octylglucoside
    		Inhibitor
    O6BTG-octylglucoside is a potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells.
  • HY-180540
    MGMT-IN-1
    		Inhibitor
    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.
  • HY-175299
    Hedgehog IN-11
    		Inhibitor
    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).
Cat. No. Product Name / Synonyms Application Reactivity