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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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 326.17. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.07 mL||15.33 mL||30.66 mL|
|5 mM||0.61 mL||3.07 mL||6.13 mL|
|10 mM||0.31 mL||1.53 mL||3.07 mL|
|50 mM||0.06 mL||0.31 mL||0.61 mL|
References are publications that support the biological activity of the product.
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 temozol. 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 temozol. resistance in human breast tumor MCF-7 cells and xenografts. Br.J.Cancer 93 1152 PMID: 16278661
Murawska et al (2022) Repurposing the damage repair protein methyl guanine methyl transferase as a ligand inducible fusion degron. ACS Chem.Biol. 17 24 PMID: 34982531
If you know of a relevant reference for Lomeguatrib, please let us know.
Keywords: Lomeguatrib, Lomeguatrib supplier, dna, mgmt, o6-methylguanine-dna, methyltransferases, inhibitors, inhibits, psuedosubstrates, epigenetics, PaTrin-2, DNA, Methyltransferases, 4359, Tocris Bioscience
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