Glucose-conjugated MGMT inhibitor

Modify Date: 2024-01-08 10:02:31

Glucose-conjugated MGMT inhibitor Structure
Glucose-conjugated MGMT inhibitor structure
Common Name Glucose-conjugated MGMT inhibitor
CAS Number 382607-78-5 Molecular Weight 616.52500
Density N/A Boiling Point N/A
Molecular Formula C24H34BrN5O7S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Glucose-conjugated MGMT inhibitor


Glucose-conjugated MGMT inhibitor is a potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells.

 Names

Name (2R,3R,4S,5S,6R)-2-[8-[2-amino-6-[(4-bromothiophen-2-yl)methoxy]purin-9-yl]octoxy]-6-(hydroxymethyl)oxane-3,4,5-triol
Synonym More Synonyms

 Glucose-conjugated MGMT inhibitor Biological Activity

Description Glucose-conjugated MGMT inhibitor is a potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells.
Related Catalog
Target

MGMT:32 nM (IC50)

In Vitro Glucose-conjugated MGMT inhibitor (O6BTG-octylglucoside) is a potent and non-toxic MGMT inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells[1].
Kinase Assay For the assays, 100 mg cell extract protein are used. In each assay, a negative and a positive sample, HeLa MR (MGMT-deficient) and HeLa S3 cell extract, respectively, are included. Incubation occurs in buffer contain-ing 700 mM HEPES-KOH (pH 7.8), 10 mM dithiothreitol and 50 mM EDTA for 90 min, which is the optimal time span for the reaction to be completed. Data are expressed as femtomoles of radioactivity trans-ferred from 3H-methylnitrosourea-labeled DNA to protein per milligram of protein within Glucose-conjugated MGMT inhibitor[1].
References

[1]. Jost Reinhard, et al. Inactivation of O6-methylguanine-DNA methyltransferase by glucose-conjugated inhibitors. Int.J.Cancer. (2001) 93,373-379.

 Chemical & Physical Properties

Molecular Formula C24H34BrN5O7S
Molecular Weight 616.52500
Exact Mass 615.13600
PSA 207.20000
LogP 1.89870
Storage condition 2-8℃

 Synonyms

Glucose-conjugated MGMT inhibitor
CS-0463