Lomeguatrib

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Cat.No. 4359 - Lomeguatrib | C10H8BrN5OS | CAS No. 192441-08-0
Description: MGMT inhibitor
Alternative Names: PaTrin-2
Chemical Name: 6-[(4-Bromo-2-thienyl)methoxy]-9H-purin-2-amine
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

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.

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

Safety Datasheet

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


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Keywords: dna mgmt o6-methylguanine-dna methyltransferases inhibitors inhibits psuedosubstrates epigenetics PaTrin-2 DNA Methyltransferases

Citations for Lomeguatrib

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases

Pathways for Lomeguatrib

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