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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
Ammonium molybdate tetrahydrate, BioReagent, suitable for cell culture, suitable for insect cell culture, 81.0-83.0% MoO3 basis
Sigma-Aldrich
Chloroform, contains ethanol as stabilizer, meets analytical specification of BP, 99-99.4% (GC)
Supelco
Hydrogen chloride – methanol solution, ~1.25 m HCl (T), derivatization grade (GC derivatization), LiChropur
Sigma-Aldrich
Chloroform, contains 100-200 ppm amylenes as stabilizer, ≥99.5%
Sigma-Aldrich
Ammonium molybdate tetrahydrate, ACS reagent, 99.98% trace metals basis
Sigma-Aldrich
Chloroform, ACS spectrophotometric grade, ≥99.8%, contains 0.5-1.0% ethanol as stabilizer
Sigma-Aldrich
Chloroform, biotech. grade, ≥99.8%, contains 0.5-1.0% ethanol as stabilizer
Sigma-Aldrich
Chloroform, ReagentPlus®, ≥99.8%, contains 0.5-1.0% ethanol as stabilizer
Sigma-Aldrich
Hydrochloric acid, puriss., 24.5-26.0%
Sigma-Aldrich
Ammonium molybdate tetrahydrate, ACS reagent, 81.0-83.0% MoO3 basis
Sigma-Aldrich
Hydrogen chloride solution, 2.0 M in diethyl ether
Sigma-Aldrich
Hydrochloric acid, 37 wt. % in H2O, 99.999% trace metals basis
Sigma-Aldrich
Chloroform, puriss. p.a., reag. ISO, reag. Ph. Eur., 99.0-99.4% (GC)
Sigma-Aldrich
Chloroform, contains amylenes as stabilizer, ACS reagent, ≥99.8%
Sigma-Aldrich
Chloroform, suitable for HPLC, ≥99.8%, amylene stabilized
Sigma-Aldrich
Chloroform, HPLC Plus, for HPLC, GC, and residue analysis, ≥99.9%, contains 0.5-1.0% ethanol as stabilizer
Sigma-Aldrich
Hydrogen chloride solution, 1.0 M in acetic acid
Sigma-Aldrich
Hydrogen chloride solution, 1.0 M in diethyl ether
Supelco
Hydrogen chloride – 2-propanol solution, ~1.25 M HCl (T), LiChropur
Sigma-Aldrich
Chloroform, contains ethanol as stabilizer, ACS reagent, ≥99.8%
Supelco
Chloroform, Pharmaceutical Secondary Standard; Certified Reference Material
Supelco
Chloroform, analytical standard
Sigma-Aldrich
DL-Dithiothreitol, BioUltra, ≥99.5% (RT)
Sigma-Aldrich
DL-Dithiothreitol, ≥99.0% (RT)
Supelco
Hydrogen chloride – ethanol solution, ~1.25 M HCl, LiChropur
Sigma-Aldrich
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
DL-Dithiothreitol, ≥98% (HPLC), ≥99.0% (titration)
Sigma-Aldrich
DL-Dithiothreitol, BioXtra, ≥99.0% (titration)
Sigma-Aldrich
DL-Dithiothreitol, ≥98% (HPLC), ≥99% (titration)
Sigma-Aldrich
Chloroform, ≥99%, PCR Reagent, contains amylenes as stabilizer