Bafilomycin-A1-minus-Bafilomycin-A1-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBafilomycin A1Cat. No.: HY-100558CAS No.: 88899-55-2Synonyms: (-)-Bafilomycin A1分式: CHO分量: 622.83作靶點: Proton Pump; Autophagy作通路: Membrane Transporter/Ion Channel; Autophagy儲存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 m

2、onth溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (160.56 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.01 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.01 mM); Suspended solution; Need ultrasonic3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/3

3、 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (4.01 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Bafilomycin A1，種從鏈霉屬物種中分離的環(huán)內(nèi)酯類抗素，是特異的 vacuolar-type H+ ATPase (V-ATPase) 抑制劑。Bafilomycin A1 抑制噬 1。IC50 & Target H+ ATPase 1體外研究 Bafilomycin A1 at a low concentration (1 nM) effectively

4、 and specifically inhibits and kills pediatric B-cellacute lymphoblastic leukemia cells. It targets both early and late stages of the autophagy pathway,mitochondria and induces caspase-independent apoptosis. Bafilomycin A1 induces the binding of Beclin 1 toBcl-2, which further inhibits autophagy and

5、 promotes apoptotic cell death 1. The growth of the BEL-7402hepatocellular carcinoma and HO-8910 ovarian cancer cell lines are retarded and the metastatic potential isinhibited by Bafilomycin A1. Transmission electron microscopy and assays of capsase-3 and -9 suggest thatBafilomycin A1 induces apopt

6、osis 2. Bafilomycin A1 inhibits the growth of a variety of cultured cells dose-dependently, including golden hamster embryo and NIH-3T3 fibroblasts, whether or not they are transformed,and PC12 and HeLa cells. The IC50 of Bafilomycin A1 for inhibition of cell growth ranges from 10 to 50 nM3.體內(nèi)研究 Chr

7、onic treatment with low-dose Bafilomycin A1 (0.1 mg/kg) slightly inhibits the tumor volume, but the finaltumor volume does not differ significantly from the control. However, chronic treatment with high doseBafilomycin A1 (1 mg/kg) inhibits the tumor growth significantly, compared with controls, aft

8、er 21 days 4.PROTOCOLCell Assay 2 Cells are harvested using 0.05% trypsin and suspended in culture medium containing 10% FCS, and 200 Lsuspension is added to each well of a 96-well plate. Cells are cultured for 20 h for adhesion. Bafilomycin A1is added to the wells at the final concentrations of 200

9、, 400 and 800 nM, in triplicate. At 24, 48 and 72 h, 20l WST-1 is added to the cells. Following incubation at 37C for 4 h, the plates are read to determine theoptical density (OD) at 435 nm with 675 nm reference using a spectrophotometer 2.MCE has not independently confirmed the accuracy of these me

10、thods. They are for reference only.Animal Mice: Tumor-bearing mice are divided randomly into three experimental groups: a low-dose Bafilomycin A1Administration 4 (0.1 mg/kg per day)-treated group (n=5), a high-dose Bafilomycin A1 (1 mg/kg per day)-treated group(n=5),and a control group (n=5). Tumor

11、size is measured and tumor volume doubling time is calculated 4.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 Adv Funct Mater. 2019 Mar. Autophagy. 2019 Jun;15(6):1017-1030.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Autophagy. 2019

12、Mar 25:1-17. Theranostics. 2019 Jul 9;9(17):4878-4892. Theranostics 2018; 8(19):5434-5451.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Yuan N, et al. Bafilomycin A1 targets both autophagy and apoptosis pathways in pediatric B-cell acute lymphoblastic leukemia.Haematologica.

13、2015 Mar;100(3):345-56.2. Lu X, et al. Bafilomycin A1 inhibits the growth and metastatic potential of the BEL-7402 liver cancer and HO-8910 ovarian cancer celllines and induces alterations in their microRNA expression. Exp Ther Med. 2015 Nov;10(5):1829-1834.3. Ohkuma S, et al. Inhibition of cell growth by bafilomycin A1, a selective inhibitor of vacuolar H(+)-ATPase. In Vitro Cell Dev Biol Anim.1993 Nov;29A(11):862-6.4. Ohta T, et al. Bafilomycin A1 induces apoptosis in the human pancreatic cancer cell line Capan-1. J Pathol. 1998 Jul;185(3):3