Lomeguatrib

Biological Activity

Lomeguatrib (LomG) is a potent inhibitor of O⁶-methylguanine-DNA methyltransferase (MGMT); (IC₅₀ = 0.009 μM in cell-free extracts from HeLa S3 cells); LomG attenuates MGMT activity in vitro and in vivo. LomG enhances the antitumor activity of temozolomide (Cat. No. 2706) in both human melanoma and MCF-7 xenografts. LomG acts as a pseudosubstrate for MGMT and can be used to induce rapid ubiquitin proteasome pathway degradation of proteins that have a MGMT fusion.

Technical Data

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.

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 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
3. O⁶-(4-bromothenyl)guanine reverses temozol. resistance in human breast tumor MCF-7 cells and xenografts.
   Clemons et al.
   Br.J.Cancer, 2005;93:1152

Product Datasheets