Drug intelligence / Profile preview

bafilomycin B1

Development stage
Unknown
Lead developer
Adipogen Life Sciences
Modality
RNA-Targeting Small Molecules → Nucleic Acid-Directed Small Molecules → Small Molecules
01

Overview

Bafilomycin B1 is a naturally occurring macrolide antibiotic produced by certain strains of Streptomyces bacteria such as Streptomyces hygroscopicus and Streptomyces lohii[1][5][7]. It is a member of the bafilomycin family of plecomacrolide antibiotics characterized by a 16-membered lactone ring[6]. Bafilomycin B1 acts as a highly specific inhibitor of vacuolar-type H+-ATPase (V-ATPase), an enzyme responsible for acidifying intracellular compartments like lysosomes and endosomes[1][5]. By inhibiting V-ATPase activity, it disrupts acidification within these organelles and impairs processes dependent on acidic pH such as protein degradation and autophagy. This mechanism has made it widely used in research to study autophagic flux and lysosomal function. In addition to its use as a research tool in cell biology and autophagy studies[3], bafilomycin B1 exhibits broad-spectrum antimicrobial activity against bacteria (especially Gram-positive), fungi, insects, nematodes, protozoans[4], with reported antitrypanosomal and antileishmanial effects[5]. However, due to general toxicity concerns and lack of clinical development or approval for human use[2], its application remains experimental.

Other names
setamycinbafilomycin-B1bafilomycin-B-1bafilomycin-B 188899-56-3CHEMBL1076858CHEMBL-1076858CHEMBL 1076858DTXSID901023400DTXSID-901023400DTXSID 901023400HY-N6738HY-N-6738HY-N 6738AKOS030213159AKOS-030213159AKOS 030213159CS-0099774CS0099774CS 0099774G17634G-17634G 17634
02

Targets

Vacuolar-type H+-ATPase c-ring

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