Bafilomycin A1

SKU: orb1223740

Description

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

Key Properties

• CAS Number: 88899-55-2
• MW: 622.83
• Purity: >98% (HPLC)
• Formula: C??H??O?
• SMILES: O[C@H]([C@H](C)/C=C(C)/C=C1OC)[C@@H](C)C/C(C)=C/C=C\[C@H](OC)C([C@@H](C)[C@H]([C@@H]([C@@]2(O)C[C@@H](O)[C@H](C)[C@@H]([C@H](C)C)O2)C)O)OC/1=O
• Target: Proton Pump

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NSC 381866

Quick Database Links

Gene Symbol

Proton Pump