Catalog Number: 4359
Alternate Names: PaTrin-2
Chemical Name: 6-[(4-Bromo-2-thienyl)methoxy]-9H-purin-2-amine
Biological Activity
Inhibitor of O6-methylguanine-DNA methyltransferase (MGMT); (IC50 = 0.009 μM in cell-free extracts from HeLa S3 cells); attenuates MGMT activity in vitro and in vivo. Enhances the antitumor activity of temozolomide (Cat. No. 2706) in both human melanoma and MCF-7 xenografts.
Technical Data
  • M.Wt:
    326.17
  • Formula:
    C10H8BrN5OS
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    192441-08-0
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Monosaccharide-linked inhibitors of O6-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships.
    Reinhard et al.
    J.Med.Chem., 2001;44:4050
  2. Sensitization of a human ovarian cancer cell line to temozolomide by simultaneous attenuation of the Bcl-2 antiapoptotic protein and DNA repair by O6-alkylguanine-DNA alkyltransferase.
    Barvaux et al.
    Mol.Cancer Ther., 2004;3:1215
  3. O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumor MCF-7 cells and xenografts.
    Clemons et al.
    Br.J.Cancer, 2005;93:1152

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