OSU-T315 _Integrin-Linked Kinase 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEOSU-T315Cat. No.: HY-18676CAS No.: 2070015-22-2分式: CHFNO分量: 533.59作靶點(diǎn): Integrin; Autophagy; Apoptosis作通路: Cytoskeleton; Autophagy; Apoptosis儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 5

2、0 mg/mL (93.70 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.17 mg/mL (4.07 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.17 mg/mL (4.07 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 OSU-T315整聯(lián)蛋連接激酶 (ILK) 的抑制劑 (IC50=0.6 M),

3、 通過(guò)去磷酸化 AKT-Ser473 和其他 ILK 靶標(biāo) (GSK-3和肌球蛋輕鏈) 抑制 PI3K/AKT 信號(hào)傳導(dǎo)。OSU-T315 阻 AKT 轉(zhuǎn)位到脂筏消除 AKT 的活化，并以ILK 依賴(lài)性式觸發(fā) Caspase 依賴(lài)性細(xì)胞凋亡 (Apoptosis)。OSU-T315 通過(guò)噬 (Autophagy) 和凋亡 (Apoptosis) 導(dǎo)致細(xì)胞死亡。IC50 & Target IC50: 0.6M; Integrin-linked kinase (ILK) inhibitor 1體外研究 OSU-T315 (Compound 22; 0-5 M; 24 hours) exhibits

4、 high in vitro potency against a panel of prostate andbreast cancer cell lines with a IC50 range of 1-2.5 M 1.OSU-T315 (0-4 M; 24 hours) can reduce YB-1, HER2, and EGFR expression; shows a modest suppressiveeffect on phosphorylated S6 levels, exhibits dose-dependent suppressive effects on the levels

5、 of phospho-ERK1/2 and phospho-p38, while that of phospho-JNK remains unaltered in PC-3 cell 1.OSU-T315 (0-4 M; 24 hours) causes autophagy through ILK inhibition 1.Cell Viability Assay 1Cell Line: Prostate cancer cells: LNCaP, PC-3; breast cancer cells: MDA-MB-231, MDA-MB-468,SKBR3, MCF-7; PrEC and

6、MEC cellsConcentration: 0-5 MIncubation Time: 24 hoursResult: Suppressed cancer cells viability in breast and prostate cancer cells (IC (50), 1-2.5M).Western Blot Analysis 1Cell Line: PC-3 cells; MDA-MB-231 cellsConcentration: 1 M, 2 M, 3 M, 4 M; 0.5 M, 1 M, 1.5 M, 2 M, 2.5 MIncubation Time: 24 hour

7、sResult: Exhibited a dose-dependent decreasing effect on the phosphorylation of pS6, ERKs, andp38 in PC-3 cells and MDA-MB-231 cells.Apoptosis Analysis 1Cell Line: PC-3 cellsConcentration: 1 M, 2 M, 3 M, 4 MIncubation Time: 24 hoursResult: Induced accumulation of LC3-II and PARP cleavage.2/3 Master

8、of Small Molecules 您邊的抑制劑師www.MedChemE體內(nèi)研究 OSU-T315 (Oral gavage; 25 mg/kg, 50 mg/kg; single daily; 35 days) has a suppressive effect of on PC-3xenograft tumor growth 1.No other obvious toxicity is observed in mice 1.Animal Model: Male NCr athymic nude mice with PC-3 tumor xenograftsDosage: 25 mg/kg

9、; 50 mg/kgAdministration: Oral gavage; single daily; 35 daysResult: Resulted in suppression of tumor growth relative to the vehicle control after 35 days oftreatment (48% and 62% suppression for 25 and 50 mg/kg, respectively).戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cancer Sci. 2019 May.See more customer validations on HYPERLIN

10、K / www.MedChemEREFERENCES1. Su-Lin Lee,et al Identification and Characterization of a Novel Integrin-Linked Kinase Inhibitor.J Med Chem. 2011 Sep 22; 54(18):636463742. Liu TM, et al. OSU-T315: a novel targeted therapeutic that antagonizes AKT membrane localization and activation of chroniclymphocytic leukemia cells. Blood. 2015 Jan 8;125(2):284-95.McePdfHeightCaution: Product has not been fully v