Pricing Availability   Qty
Description: MGMT inhibitor
Alternative Names: PaTrin-2
Chemical Name: 6-[(4-Bromo-2-thienyl)methoxy]-9H-purin-2-amine
Purity: ≥98% (HPLC)
Literature (3)

Biological Activity for Lomeguatrib

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.

Technical Data for Lomeguatrib

M. Wt 326.17
Formula C10H8BrN5OS
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 192441-08-0
PubChem ID 3025944
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Lomeguatrib

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 32.62 100

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 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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.


Dilution Calculator

Calculate the dilution required to prepare a stock solution.

References for Lomeguatrib

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.

View Related Products by Target

View Related Products by Product Action

View all DNA Methyltransferase Inhibitors

Keywords: Lomeguatrib, Lomeguatrib supplier, dna, mgmt, o6-methylguanine-dna, methyltransferases, inhibitors, inhibits, psuedosubstrates, epigenetics, PaTrin-2, DNA, Methyltransferases, 4359, Tocris Bioscience

Citations for Lomeguatrib

Citations are publications that use Tocris products.

Currently there are no citations for Lomeguatrib. Do you know of a great paper that uses Lomeguatrib from Tocris? Please let us know.

Reviews for Lomeguatrib

There are currently no reviews for this product. Be the first to review Lomeguatrib and earn rewards!

Have you used Lomeguatrib?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Cell Cycle and DNA Damage Research Product Guide

Cell Cycle and DNA Damage Research Product Guide

This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:

  • Cell Cycle and Mitosis
  • DNA Damage Repair
  • Targeted Protein Degradation
  • Ubiquitin Proteasome Pathway
  • Chemotherapy Targets
Epigenetics in Cancer Research Product Guide

Epigenetics in Cancer Research Product Guide

This product guide reviews some of the main areas in cancer epigenetics research and lists around 120 products that can be used for the main epigenetic targets including:

  • Histone Methylation
  • Histone Acetylation
  • DNA Methylation
  • Ubiquitination
  • Bromodomains
Epigenetics Scientific Review

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.