Chemical Name: 6-[(4-Bromo-2-thienyl)methoxy]-9H-purin-2-amine
Biological ActivityLomeguatrib is an 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.
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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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