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Merck

Targeting PTEN using small molecule inhibitors.

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

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
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Sigma-Aldrich
Hydrochloric acid, meets analytical specification of Ph. Eur., BP, NF, fuming, 36.5-38%
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Hydrochloric acid, ACS reagent, 37%
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Hydrochloric acid solution, 1.0 N, BioReagent, suitable for cell culture
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Hydrochloric acid solution, ~6 M in H2O, for amino acid analysis
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Hydrochloric acid, puriss. p.a., ACS reagent, reag. ISO, reag. Ph. Eur., fuming, ≥37%, APHA: ≤10
Supelco
Hydrochloric acid solution, volumetric, 0.1 M HCl (0.1N), endotoxin free
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Hydrochloric acid, ACS reagent, 37%
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Hydrogen chloride solution, 4.0 M in dioxane
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Hydrochloric acid, BioReagent, 36.5-38.0%
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Hydrochloric acid solution, 32 wt. % in H2O, FCC
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Malachite Green oxalate salt, Technical grade
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Chloroform, contains 100-200 ppm amylenes as stabilizer, ≥99.5%
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Chloroform, analytical standard
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Chloroform, anhydrous, contains amylenes as stabilizer, ≥99%
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Chloroform, Pharmaceutical Secondary Standard; Certified Reference Material
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Chloroform, ≥99%, PCR Reagent, contains amylenes as stabilizer
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Chloroform, ReagentPlus®, ≥99.8%, contains 0.5-1.0% ethanol as stabilizer
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Chloroform, ACS spectrophotometric grade, ≥99.8%, contains 0.5-1.0% ethanol as stabilizer
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Chloroform, HPLC Plus, for HPLC, GC, and residue analysis, ≥99.9%, contains amylenes as stabilizer
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Ammonium molybdate, meets USP testing specifications
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Ammonium molybdate, 99.98% trace metals basis
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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
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Chloroform, contains ethanol as stabilizer, meets analytical specification of BP, 99-99.4% (GC)
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