Bafilomycin A1 belongs to the macrolide class of antibiotics and is a V-ATPase inhibitor (IC50=0.44 nM) that is specific and reversible. Bafilomycin A1 is an inhibitor of the late phase of autophagy, blocking the fusion of autophagosomes with lysosomes. Bafilomycin A1 also induces apoptosis.

METHODS: Human pancreatic cancer cells Capan-1 were treated with Bafilomycin A1 (1-100 nM) for 72 h. Cell growth inhibition was detected using MTT.
RESULTS: Bafilomycin A1 dose-dependently inhibited the growth of Capan-1 cells with an IC50 of 5 nM. [1]
METHODS: Human osteosarcoma cells MG63 were treated with Bafilomycin A1 (1 μmol/L) for 6-24 h. The expression levels of target proteins were detected by Western Blot.
RESULTS: Bafilomycin A1 induced a significant increase in the levels of apoptosis-related proteins p53 and Beclin 1, a significant decrease in the expression of autophagy-related proteins p62 and LC3-I, and an increase in LC3-II. [2]
METHODS: Human hepatocellular carcinoma cells BEL7402 and HepG2 were incubated with Bafilomycin A1 (5 nM) for 24 h, and the cell cycle was examined by Flow Cytometry.
RESULTS: Bafilomycin A1 increased the percentage of BEL7402 and HepG2 cells in the G1 phase of the cell cycle, while cells in the G2/M phase decreased, indicating G1 phase arrest. [3]

METHODS: To assay antitumor activity in vivo, Bafilomycin A1 (0.1-1 mg/kg) was intraperitoneally injected once daily for three days into NOD-SCID mice harboring the human acute lymphoblastic leukemia tumor B-ALL.
RESULTS: Bafilomycin A1 prolonged the survival and improved the pathology of xenograft mice by targeting leukemia cells. [4]
METHODS: To investigate the role of autophagy in chronic wound healing, Bafilomycin A1 (1 mg/kg) was administered as a single intraperitoneal injection to diabetic db/db mice.
RESULTS: Bafilomycin A1 treatment significantly accelerated wound healing in db/db mice and exerted a favorable healing effect.Bafilomycin A1 may accelerate the healing of diabetic chronic refractory wounds by promoting cell proliferation, collagen production, and modulating inflammatory homeostasis. [5]