382607-78-5

382607-78-5 structure

Name: Glucose-conjugated MGMT inhibitor
Chemical 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
CAS Number: 382607-78-5
Molecular Formula: C₂₄H₃₄BrN₅O₇S
Molecular Weight: 616.52500
Catalog: Signaling Pathways Epigenetics DNA Methyltransferase
Create Date: 2016-02-11 18:53:37
Modify Date: 2024-01-08 10:02:31
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.

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
Synonyms	Glucose-conjugated MGMT inhibitor CS-0463

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	Signaling Pathways >> Epigenetics >> DNA Methyltransferase Research Areas >> Cancer
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.