Lomeguatrib

Name: Lomeguatrib
Brand: Tocris Bioscience
SKU: 4359

Tocris Bioscience, part of Bio-Techne | Catalog # 4359

COA / SDS

MGMT inhibitor

Key Product Details

Description:	MGMT inhibitor
Alternative Names:	PaTrin-2
Chemical Name:	6-[(4-Bromo-2-thienyl)methoxy]-9H-purin-2-amine
Purity:	≥98% (HPLC)
Molecular Weight:	326.17

View Full Technical Details for Lomeguatrib

Technical Data
Citations

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
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.

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

Solubility for Lomeguatrib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	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.

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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References for Lomeguatrib

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