Bafilomycin A1 is a macrolide antibiotic isolated from the Streptomyces species and an inhibitor of vacuolar V-ATPase.

Bafilomycin A1 at a low concentration (1 nM) effectively and specifically inhibits and kills pediatric B-cell acute 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 to Bcl-2, which further inhibits autophagy and promotes apoptotic cell death^[1]. The growth of the BEL-7402 hepatocellular carcinoma and HO-8910 ovarian cancer cell lines are retarded and the metastatic potential is inhibited by bafilomycin A1. Transmission electron microscopy and assays of capsase-3 and −9 suggest that bafilomycin A1 induces apoptosis^[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 nM^[3].

Chronic treatment with low-dose bafilomycin A1 (0.1 mg/kg) slightly inhibits the tumor volume, but the final tumor volume does not differ significantly from the control. However, chronic treatment with high dose bafilomycin A1 (1 mg/kg) inhibits the tumor growth significantly, compared with controls, after 21 days^[4].

• [1]. Yuan N, et al. Bafilomycin A1 targets both autophagy and apoptosis pathways in pediatric B-cell acute lymphoblastic leukemia. Haematologica. 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 cell lines 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):324-30.

Cells are harvested using 0.05% trypsin and suspended in culture medium containing 10% FCS, and 200 µL suspension is added to each well of a 96-well plate. Cells are cultured for 20 h for adhesion. Bafilomycin A1 is added to the wells at the final concentrations of 200, 400 and 800 nM, in triplicate. At 24, 48 and 72 h, 20 µl WST-1 is added to the cells. Following incubation at 37°C for 4 h, the plates are read to determine the optical density (OD) at 435 nm with 675 nm reference using a spectrophotometer^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Mouse: Tumor-bearing mice are divided randomly into three experimental groups: a low-dose bafilomycin A1(0.1 mg/kg per day)-treated group (n=5), a high-dosebafilomycin A1(1 mg/kg per day)-treated group (n=5),and a control group (n=5). Tumor size is measured and tumor volume doubling time is calculated^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Yuan N, et al. Bafilomycin A1 targets both autophagy and apoptosis pathways in pediatric B-cell acute lymphoblastic leukemia. Haematologica. 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 cell lines 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):324-30.

622.83

C₃₅H₅₈O₉

88899-55-2

Room temperature in continental US; may vary elsewhere

DMSO

* "<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">