Chemical Name: 6-[(4-Bromo-2-thienyl)methoxy]-9H-purin-2-amine
Biological ActivityInhibitor 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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 temozol. 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 temozol. resistance in human breast tumor MCF-7 cells and xenografts.
Clemons et al.
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