Lomeguatrib

(HB1376)

Product overview

  • Name
    Lomeguatrib
  • Short description
    Potent MGMT inhibitor
  • Biological description
    Potent O6-methylguanine-DNA methyltransferase (MGMT) inhibitor (IC50 = 9 nM). Acts as a pseudosubstrate. Enhances temozolomide anti-tumor activity. Shows anti-cancer actions.
  • Alternative names
    PaTrin-2; Patrin; O6-(4-bromothenyl)guanine; 4-BTG
  • Biological action
    Inhibitor
  • Purity
    >98%
  • Citations

Properties

  • Chemical name
    6-[(4-Bromo-2-thienyl)methoxy]-9H-p urin-2-amine
  • Molecular Weight
    326.17
  • Chemical structure
    Lomeguatrib  [192441-08-0]
  • Molecular Formula
    C10H8BrN5OS
  • CAS Number
    192441-08-0

Storing and Using Your Product

  • Storage instructions
    +4°C
  • Solubility overview
    soluble in DMSO (100mM)
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

References for Lomeguatrib

  • Monosaccharide-linked inhibitors of O(6)-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships.

    Reinhard J et al (2001) J Med Chem 44(24) : 4050-61.
    PubMedID: 11708909
  • O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenografts.

    Clemons M et al (2005) Br J Cancer 93(10) : 1152-6.
    PubMedID: 16278661
  • The therapeutic potential of O6-alkylguanine DNA alkyltransferase inhibitors.

    Khan O et al (2007) Expert Opin Investig Drugs 16(10) : 1573-84.
    PubMedID: 17922622

Reviews & Product Guides