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巴佛洛霉素A1;巴弗洛霉素A1

CAS No. : 88899-55-2

MCE 国际站：Bafilomycin A1

产品活性：Bafilomycin A1 (BafA1) 是特异性，可逆的 V-ATPase 抑制剂，IC₅₀ 值为 4-400 nmol/mg。Bafilomycin A1，大环内酯类抗生素，是一种自噬 (autophagy) 晚期阶段抑制剂。Bafilomycin A1 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。Bafilomycin A1 也诱导调亡 (apoptosis)。

研究领域：Membrane Transporter/Ion Channel | Autophagy | Anti-infection | Apoptosis

作用靶点：Proton Pump | Autophagy | Antibiotic | Bacterial | Apoptosis

结构分类：抗生素 | 大环内脂类

In Vitro: Bafilomycin A1 is treated to different types of membrane ATPases with the I₅₀ of 400 nmol/mg, 4 nmol/mg ａnd 50 nmol/mg for the vacuolar ATPases of a fungus (N. crassa), a plant (Z. mays), ａnd an animal (bovine abrenal medulla). The I₅₀ values refer as μmol of Bafilomycin A1 per mg of protein giving 50% inhibition of ATPase activity.
Bafilomycin A1 ((-)-Bafilomycin A1) disrupts autophagic flux by inhibiting both V-ATPase-dependent acidification ａnd Ca-P60A/SERCA-dependent autophagosome-lysosome fusion.
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.
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.
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.

In Vivo: 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.
Bafilomycin A1 (0.1 mg/kg or 1 mg/kg; i.p. daily for 3 days) extends the survival of B-cell acute lymphoblastic leukemia (B-ALL) xenograft mice with advanced disease.