Cat. No. 4359
Alternative Name: PaTrin-2
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.
Certificate of Analysis / Safety Data Sheet
Reinhard et al (2001) Monosaccharide-linked inhibitors of O6-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships. J.Med.Chem. 44 4050. PMID: 11708909.
Barvaux et al (2004) 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. Mol.Cancer Ther. 3 1215. PMID: 15486188.
Clemons et al (2005) O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumor MCF-7 cells and xenografts. Br.J.Cancer 93 1152. PMID: 16278661.
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Keywords: Lomeguatrib, supplier, dna, mgmt, o6-methylguanine-dna, methyltransferases, inhibitors, psuedosubstrates, epigenetics
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