Targeting PTEN using small molecule inhibitors.

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

366927

Sigma-Aldrich

Chloroform, suitable for HPLC, ≥99.8%, contains 0.5-1.0% ethanol as stabilizer

650471

Sigma-Aldrich

Chloroform, HPLC Plus, for HPLC, GC, and residue analysis, ≥99.9%, contains 0.5-1.0% ethanol as stabilizer

650498

Sigma-Aldrich

Chloroform, HPLC Plus, for HPLC, GC, and residue analysis, ≥99.9%, contains amylenes as stabilizer

W530574

Sigma-Aldrich

Hydrochloric acid solution, 32 wt. % in H₂O, FCC

07102

Sigma-Aldrich

Hydrochloric acid, meets analytical specification of Ph. Eur., BP, NF, fuming, 36.5-38%

A7302

Sigma-Aldrich

Ammonium molybdate tetrahydrate, ACS reagent, 81.0-83.0% MoO₃ basis

319988

Sigma-Aldrich

Chloroform, contains ethanol as stabilizer, ACS reagent, ≥99.8%

320331

Sigma-Aldrich

Hydrochloric acid, ACS reagent, 37%

304174

Sigma-Aldrich

Hydrogen chloride solution, 1.0 M in acetic acid

294837

Sigma-Aldrich

Hydrogen chloride solution, 1.0 M in diethyl ether

455180

Sigma-Aldrich

Hydrogen chloride solution, 2.0 M in diethyl ether

366919

Sigma-Aldrich

Chloroform, ACS spectrophotometric grade, ≥99.8%, contains 0.5-1.0% ethanol as stabilizer

345547

Sigma-Aldrich

Hydrogen chloride solution, 4.0 M in dioxane

339253

Sigma-Aldrich

Hydrochloric acid, 37 wt. % in H₂O, 99.999% trace metals basis

24216

Sigma-Aldrich

Chloroform, contains ethanol as stabilizer, meets analytical specification of BP, 99-99.4% (GC)

472476

Sigma-Aldrich

Chloroform, contains amylenes as stabilizer, ACS reagent, ≥99.8%

496189

Sigma-Aldrich

Chloroform, biotech. grade, ≥99.8%, contains 0.5-1.0% ethanol as stabilizer

431346

Sigma-Aldrich

Ammonium molybdate tetrahydrate, for inorganic trace analysis, ACS reagent, 99.98% trace metals basis

C2432

Sigma-Aldrich

Chloroform, contains 100-200 ppm amylenes as stabilizer, ≥99.5%

258148

Sigma-Aldrich

Hydrochloric acid, ACS reagent, 37%

PHR1552

Supelco

Chloroform, Pharmaceutical Secondary Standard; Certified Reference Material

T4174

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

A1343

Sigma-Aldrich

Ammonium molybdate, meets USP testing specifications

705551

Sigma-Aldrich

Hydrogen chloride solution, 3 M in cyclopentyl methyl ether (CPME)

372978

Sigma-Aldrich

Chloroform, anhydrous, contains amylenes as stabilizer, ≥99%

277908

Sigma-Aldrich

Ammonium molybdate, 99.98% trace metals basis