LYN-1604-LYN1604-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELYN-1604Cat. No.: HY-101923CAS No.: 2088939-99-3Synonyms: LYN1604; LYN 1604分式: CHClNO分量: 584.62作靶點(diǎn): ULK; Autophagy作通路: Autophagy儲(chǔ)存式: Please store the product under the recommended conditions inthe COA.溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL

2、(171.05 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.7105 mL 8.5526 mL 17.1051 mL5 mM 0.3421 mL 1.7105 mL 3.4210 mL10 mM 0.1711 mL 0.8553 mL 1.7105 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 LYN-1604種有效的 UNC-51 樣激酶 1 (ULK1) 激動(dòng)劑，其 EC50

3、 值為 18.94 nM。IC50 & Target EC50: 18.94 nM (ULK1) 1體外研究LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) agonist with an EC50 of 18.94 nM in ADP-Glo kinaseassay. The in vitro kinase assay reveals that the LYN-1604 increases the phosphorylation of mATG13 atser318 in wild-type ULK1 transfected HEK-293T

4、cells. It is found that LYN-1604-treated cells display aremarkable green fluorescence with MDC staining and the autophagy ratio is increased in a dose-dependent1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEmanne. It is also found that LYN-1604 induces remarkable up-regulation of Beclin-1 and degr

5、adation of p62,as well as transformation of LC3-I to LC3-II 1.體內(nèi)研究 Based on the results of tumor volume and weight, it is found that LYN-1604 can significantly inhibit thegrowth of xenograft MDA-MB-231 cells. The body weights of mice are stable, with no obvious distinctionsbetween LYN-1604-treated a

6、nd control mice. It also reveals that LYN-1604 induces remarkable autophagy invivo 1.PROTOCOLKinase Assay 1 Cells or tumor tissues are treated with LYN-1604 for the indicated times. Both adherent and floating cells arecollected and western blot analysis is carried out. Briefly, the cell pellets ae r

7、esuspended with lysis bufferconsisting of 50 mM HEPES, pH 7.4; 1% Triton-X-100, 2 mM sodium orthovanadate, 100 mM sodiumfluoride, 1 mM edetic acid, 1 mM PMSF, 10 mg/L aprotinin and 10 mg/Lleupeptin, and lysed at 4C for 1 h.After 12000 rpm centrifugation for 15 min, the protein content of the superna

8、tant is determined by the Bio-Rad DC protein assay 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 Cells are dispensed in 96-well plates at a density of 5104 cells per mL. After 24 h of incubation, cells aretreated with different concentr

9、ations of LYN-1604 for the indicated time periods. Cell viability is measured bythe MTT assay 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal 24 female nude mice (BALB/c, 6 to 8 weeks, 20 to 22 g) are used and injected subcutaneously with MDA-A

10、dministration 1 MB-231 cells (5106 cells per mouse). When the tumors reach 100 mm3 in volume (V=LW2/2), the miceare divided into four groups. Three groups are treated with different doses of LYN-1604 once a day byintragastric administration for 14 days (low dose, 25 mg/kg; median dose, 50 mg/kg; hig

11、h dose, 100 mg/kg),whereas the control group is treated with vehicle control. During the treatment, the tumor volumes and bodyweight are measured every day until the end of the study. At the end of treatment, all mice are sacrificed. Thespleen, liver, kidney and tumor tissue are harvested, weighed,

12、and photographed, then immediately frozen inliquid nitrogen or fixed in formalin 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Biochem J. 2019 Mar 12;476(5):875-887.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Zhang L, et al. Discovery of a small molecule targeting ULK1-modulated cell death of triple negative breast cancer in vitro and in vivo.Chem Sci. 2017 Apr 1;8(4):2687-2701.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMcePdfHeigh