Lomeguatrib

Key Product Details

Product Description

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.

Product Specifications for Lomeguatrib

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for Lomeguatrib

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Murawska Repurposing the damage repair protein methyl guanine methyl transferase as a ligand inducible fusion degron. ACS Chem.Biol. 2022 PMID: 34982531
• Barvaux 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. 2004 PMID: 15486188
• Clemons O⁶-(4-bromothenyl)guanine reverses temozol. resistance in human breast tumor MCF-7 cells and xenografts. Br.J.Cancer 2005 PMID: 16278661
• Reinhard Monosaccharide-linked inhibitors of O⁶-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships. J.Med.Chem. 2001 PMID: 11708909

Product Documents for Lomeguatrib