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Merck

Targeting PTEN using small molecule inhibitors.

Methods (San Diego, Calif.) (2015-03-10)
Lok Hang Mak, Rudiger Woscholski
ABSTRACT

PTEN (phosphatase and tensin homologue deleted on chromosome 10) is well known as a tumour suppressor. It's PI(3,4,5)P3 lipid phosphatase activity is an important counteracting mechanism in PI 3-kinase (phosphoinositide 3-kinase) signalling. Furthermore, PTEN lies upstream of Akt kinase, a key enzyme in insulin signalling regulating glucose uptake and cell growth. Therefore, PTEN has recently gained attention as a valuable drug target for the treatment of diabetes, stroke, cardiac infarct and fertility. This review summarizes the use of small molecules as PTEN inhibitors. Currently available methodologies and techniques for accessing PTEN inhibition in vitro and in cellulo will be discussed.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
DL-Dithiothreitol, BioXtra, ≥99.0% (titration)
Sigma-Aldrich
DL-Dithiothreitol, ≥98% (HPLC), ≥99.0% (titration)
Sigma-Aldrich
Chloroform, ≥99%, PCR Reagent, contains amylenes as stabilizer
Supelco
Hydrochloric acid solution, volumetric, 0.1 M HCl (0.1N), endotoxin free
Sigma-Aldrich
Ammonium molybdate, meets USP testing specifications
Sigma-Aldrich
Ammonium molybdate, 99.98% trace metals basis
Supelco
Hydrogen chloride – methanol solution, ~1.25 m HCl (T), for GC derivatization, LiChropur
Supelco
Hydrogen chloride – ethanol solution, ~1.25 M HCl, for GC derivatization, LiChropur
Sigma-Aldrich
Dulbecco′s Modified Eagle′s Medium - low glucose, With 1000 mg/L glucose, L-glutamine, and sodium bicarbonate, liquid, sterile-filtered, suitable for cell culture
Sigma-Aldrich
Dulbecco′s Modified Eagle′s Medium - high glucose, With 4500 mg/L glucose and sodium bicarbonate, without L-glutamine and sodium pyruvate, liquid, sterile-filtered, suitable for cell culture, suitable for hybridoma
Supelco
Chloroform, analytical standard
Sigma-Aldrich
DL-Dithiothreitol, ≥99.0% (RT)
Supelco
Hydrogen chloride – 2-propanol solution, ~1.25 M HCl (T), for GC derivatization, LiChropur
Supelco
Chloroform, suitable for HPLC, ≥99.8%, contains 0.5-1.0% ethanol as stabilizer
Sigma-Aldrich
Chloroform, ACS reagent, ≥99.8%, contains 0.5-1.0% ethanol as stabilizer
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Ammonium molybdate tetrahydrate, BioUltra, ≥99.0% (T)
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Trypsin-EDTA solution, 10 ×, sterile-filtered, BioReagent, suitable for cell culture, 5.0 g porcine trypsin and 2 g EDTA, 4Na per liter of 0.9% sodium chloride
Sigma-Aldrich
Chloroform, ACS reagent, ≥99.8%, contains amylenes as stabilizer
Sigma-Aldrich
Chloroform, anhydrous, ≥99%, contains 0.5-1.0% ethanol as stabilizer
Sigma-Aldrich
Hydrogen chloride solution, 3 M in cyclopentyl methyl ether (CPME)
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Malachite Green oxalate salt, Technical grade
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Hydrochloric acid, 36.5-38.0%, BioReagent, for molecular biology
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Hydrochloric acid solution, 1.0 N, BioReagent, suitable for cell culture
Supelco
Chloroform, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
DL-Dithiothreitol, suitable for electrophoresis, ≥99%
Sigma-Aldrich
DL-Dithiothreitol, for molecular biology, ≥98% (HPLC), ≥99% (titration)
Sigma-Aldrich
Chloroform, anhydrous, contains amylenes as stabilizer, ≥99%
Sigma-Aldrich
DL-Dithiothreitol, BioUltra, for molecular biology, ≥99.5% (RT)
Sigma-Aldrich
Hydrochloric acid solution, ~6 M in H2O, for amino acid analysis
Sigma-Aldrich
Ammonium molybdate tetrahydrate, BioReagent, suitable for cell culture, suitable for insect cell culture, 81.0-83.0% MoO3 basis