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Biological Data
| Biological description | Potent O6-methylguanine-DNA methyltransferase (MGMT) inhibitor (IC50 = 9 nM). Acts as a pseudosubstrate. Enhances temozolomide anti-tumor activity. Shows anti-cancer actions. |
Solubility & Handling
| Storage instructions | +4°C |
| Solubility overview | Soluble in DMSO (100mM) |
| Important | This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use. |
Chemical Data
| Chemical name | 6-[(4-Bromo-2-thienyl)methoxy]-9H-p urin-2-amine |
| Chemical structure | ![Lomeguatrib [192441-08-0] Chemical Structure](data:image/png;base64,iVBORw0KGgoAAAANSUhEUgAAAAEAAAABCAQAAAC1HAwCAAAAC0lEQVR4nGP6zwAAAgcBApocMXEAAAAASUVORK5CYII= "Lomeguatrib [192441-08-0]") |
| Molecular Formula | C10H8BrN5OS |
| PubChem identifier | 3025944 |
| SMILES | NC1=NC(OCC3=CC(Br)=CS3)=C2C(N=CN2)=N1 |
| InChiKey | JUJPKFNFCWJBCX-UHFFFAOYSA-N |
References for Lomeguatrib
References are publications that support the biological activity of the product
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The therapeutic potential of O6-alkylguanine DNA alkyltransferase inhibitors.
Khan O et al (2007) Expert Opin Investig Drugs 16(10) : 1573-84. -
O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenografts.
Clemons M et al (2005) Br J Cancer 93(10) : 1152-6. -
Monosaccharide-linked inhibitors of O(6)-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships.
Reinhard J et al (2001) J Med Chem 44(24) : 4050-61.
![Lomeguatrib [192441-08-0] Chemical Structure](https://hellobio.com/media/catalog/product//h/b/hb1376.png "Lomeguatrib [192441-08-0]")
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