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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESF1670Cat. No.: HY-15842CAS No.: 345630-40-2Synonyms: PTPase CD45 Inhibitor分式: CHNO分量: 307.34作靶點(diǎn): PTEN; Phosphatase作通路: PI3K/Akt/mTOR; Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 mon
2、th溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (162.69 mM)H2O : 90% corn oilSolubility: 2.5 mg/mL (8.13 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 SF1670種有效的特異性的第10號(hào)染體缺失的磷酸酶及張蛋同 蛋 (PTEN) 抑制劑。IC50 & Target PTEN 1體外研究 SF1670 is a specific PTEN inhibitor with prolonged intr
3、acellular retention in neutrophils. SF1670 enhancesPtdIns(3,4,5)P3 signaling in transplanted neutrophils. SF1670 also elevates Akt phosphorylation in murinecells. Consistent with the enhanced Akt phosphorylation, pretreatment with SF1670 also significantlyaugments PtdIns(3,4,5)P3 level in mouse neut
4、rophils. SF1670-induced Akt hyperactivation is abolished inPTEN-null neutrophils, further demonstrating that this effect is mediated by specific inhibition of PTENactivity. At 500 nM fMLP stimulation, SF1670 (500 nM)pretreated neutrophils show nearly 70% higher(maximal) superoxide production than un
5、treated neutrophils 1. HCT116 cells are pre-treated with the PTENinhibitor SF1670 (2 M) for 24 h (untreated HCT116 cells served as control); treated cells are subsequentlyplated under non-adherent conditions with added MET (60 M), Lun (2 M), or Gen (2 M). SF1670 binds tothe PTEN active site, resulti
6、ng in elevated phosphatidylinositol (3,4,5) triphosphate signaling 2.PROTOCOLCell Assay 2 The human colon cancer cell lines HT29 and HCT116 are propagated in McCoys medium (ATCC)supplemented with 10 % fetal bovine serum (FBS) and 5 % antibiotic-antimycotic solution (ABAM) in ahumidified incubator (5
7、 % CO2:95 % air) at 37C. Cells are seeded in six-well plates at an initial density of2105 per well, and treated (in culture medium) with Metformin (MET 60 M), Lunasin (Lun 2 M), -conglycinin (-con 3 M), Glycinin (Gly 3 M), and Genistein (Gen 2 M), alone or in combination. -con andGly are isolated an
8、d purified as described below. Metformin, Lun, -con, and Gly are dissolved in phosphate-buffered saline (PBS), whereas Gen is dissolved in DMSO. In other experiments, cells are treated with insulin(2 M), PTEN inhibitor SF1670 (2 M), and 5-Fluorouracil (5-FU 50 M). Treated cells are collected at sele
9、cttime points for subsequent analyses 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶(hù)使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Death Dis. 2019 Mar 13;10(3):248. Eur Rev Med Pharmacol Sci. 2019 Apr;23(7):3080-3087. Mol Med Rep. 2018 Jul;18(1):349-357. Int J Clin Exp Med. 2019
10、;12(7):8739-8745. Int J Clin Exp Med. 2019;12(7):8992-8998.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Li Y, et al. Pretreatment with phosphatase and tensin homolog deleted on chromosome 10 (PTEN) inhibitor SF1670augments the2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE
11、efficacy of granulocyte transfusion in a clinically relevant mouse model. Blood. 2011 Jun 16;117(24):6702-13.2. Montales MT, et al. Metformin and soybean-derived bioactive molecules attenuate the expansion of stem cell-like epithelialsubpopulation and confer apoptotic sensitivity in human colon cancer cells. Genes Nutr. 2015 Nov;10(6):49.McePdfHeightCaution: Product has no
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