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Glucose-conjugated MGMT inhibitor

Catalog No.GC36153 Copy One-Click Copy Product Info

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.

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Glucose-conjugated MGMT inhibitor Chemical Structure

Cas No.: 382607-78-5

Size Price Stock Qty
10mM (in 1mL DMSO)
$244.00
In stock
5mg
$180.00
In stock
10mg
$270.00
In stock
50mg
$765.00
In stock

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Sample solution is provided at 25 µL, 10mM.



Description 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. MGMT|32 nM (IC50)

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].

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

Protocol of Glucose-conjugated MGMT inhibitor

Kinase experiment:

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 O6BTG-octylglucoside[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 Properties of Glucose-conjugated MGMT inhibitor

Cas No. 382607-78-5 SDF
Canonical SMILES [H][C@]1([C@]([H])(O[C@@](OCCCCCCCCN2C3=C(N=C2)C(OCC4=CC(Br)=CS4)=NC(N)=N3)([C@](O)([C@]1(O)[H])[H])[H])CO)O
Formula C24H34BrN5O7S M.Wt 616.53
Solubility DMSO: 100 mg/mL (162.20 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Glucose-conjugated MGMT inhibitor

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1 mg 5 mg 10 mg
1 mM 1.622 mL 8.1099 mL 16.2198 mL
5 mM 324.4 μL 1.622 mL 3.244 mL
10 mM 162.2 μL 811 μL 1.622 mL
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In vivo Formulation Calculator (Clear solution) of Glucose-conjugated MGMT inhibitor

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 2 reference(s) in Google Scholar.)

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