Bafilomycin A1

SKU: orb1300510

Description

Bafilomycin A1 is a specific and reversible macrolide antibiotic that potently inhibits V-ATPase (IC50=0.44 nM). It blocks autophagosome-lysosome fusion, arresting late-stage autophagy, and can induce apoptosis, making it a valuable tool for studying autophagy, cancer, and neurodegeneration in cellular and animal models.

Research Area

Cell Biology

Key Properties

• CAS Number: 88899-55-2
• MW: 622.8
• Purity: >98%
• Formula: C₃₅H₅₈O₉
• SMILES: [H][C@@]1(OC(=O)\C(OC)=C\C(\C)=C\[C@@H](C)[C@@H](O)[C@@H](C)C\C(C)=C\C=C\[C@@H]1OC)[C@@H](C)[C@@H](O)[C@H](C)[C@@]1(O)C[C@@H](O)[C@H](C)[C@H](O1)C(C)C
• Target: ATPase
• Solubility: Soluble in DMSO (up to 50 mg/ml)

Bioactivity

• Target IC50:
  Proteoglycan degradation (stimulated by IL-1):< 10 nM|V-ATPase:14 nmol /mg|short circuit current:0.17 μM
• In Vivo:
  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. 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.
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• In Vitro:
  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. 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. 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.
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Storage & Handling

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

Alternative Names

From Streptomyces griseus

Compound Identifiers

PubChem CID

6436223