Biological Activity
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.
Compound Libraries
Lomeguatrib is also offered as part of the Tocriscreen Plus and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 326.17 |
| Formula | C10H8BrN5OS |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 192441-08-0 |
| PubChem ID | 3025944 |
| InChI Key | JUJPKFNFCWJBCX-UHFFFAOYSA-N |
| Smiles | NC1=NC(OCC3=CC(Br)=CS3)=C2C(N=CN2)=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.62 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 326.17. Batch specific molecular weights may vary from batch to batch due to solvent 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 |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: Lomeguatrib, supplier, dna, mgmt, o6-methylguanine-dna, methyltransferases, inhibitors, inhibits, psuedosubstrates, epigenetics, PaTrin-2, DNA, Methyltransferases, DNA, Methyltransferases, Tocris Bioscience
