Inhibitor of O6
-methylguanine-DNA methyltransferase (MGMT); (IC50
= 0.009 μ
M 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.
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.
Monosaccharide-linked inhibitors of O6-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships.
Reinhard et al.
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
O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumor MCF-7 cells and xenografts.
Clemons et al.