Bafilomycin A1 是可逆特异性V-ATPase抑制剂，IC50值为 4-400 nmol/mg。它阻断自噬体与溶酶体的融合，并抑制培养细胞溶酶体中的酸化和蛋白质降解。它是大环内酯类抗生素， 也是自噬晚期阶段抑制剂。它也诱导调亡 。

Bafilomycin A1 induces caspase-independent cell death in hepatocellular carcinoma cells via targeting of autophagy and MAPK pathways. Bafilomycin A1 is a vacuolar H+-ATPase inhibitor (IC50: 0.44 nM). It is also found to inhibit autophagy while induces apoptosis.Bafilomycin A1 triggers proliferative potential of senescent cancer cells in vitro and in NOD/SCID mice.

Bafilomycin A1 at a concentration of 1 nM effectively and specifically kills pediatric B-cell acute lymphoblastic leukemia cells. 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, NIH-3T3 fibroblasts, PC12 and HeLa cells. The IC50 of Bafilomycin A1 for inhibition of cell growth ranges from 10 to 50 nM[3].

Chronic treatment with Bafilomycin A1 at the dose of 1 mg/kg significantly inhibits the tumor growth compared with controls, after 21 days[4].

88899-55-2

C35H58O9

622.83

巴佛洛霉素A1;巴佛洛霉素 A1

DMSO:99 mg/mL(158.95 mM)
H2O:0.1 mg/mL (0.16 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years