88899-55-2

white to off-white powder

A macrolide antibiotic and potent and selective inhibitor of vacuolar-type (v-type) H+ ATPase

Bafilomycin A1 is a member of a potent family of macrocyclic lactones with broad spectrum biological activity, including activity against bacteria, yeast, fungi, nematodes, insects and tumor cell lines. Bafilomycin A1 is an inhibitor of vacuolar-type ATPase.

Bafilomycin A1 is a member of a potent family of macrocyclic lactones with broad spectrum biological activity, including activity against bacteria, yeast, fungi, nematodes, insects and tumour cell lines. Bafilomycin A1 is an inhibitor of vacuolar-type ATPase.

ChEBI: The most used of the bafilomycins, a family of toxic macrolide antibiotics derived from Streptomyces griseus.

Highly potent, selective inhibitor of vacuolar H + -ATPases (IC 50 = 500 pM as measured in chromaffin granule membranes). Selective over other ATP hydrolyzing enzymes such as F-ATPases, Ca 2+ -ATPases, Na + /K + -ATPases and plasma membrane H + -ATPases.

Bafilomycin A₁ is a fungal metabolite that has been found in Streptomyces and has diverse biological activities. It is an inhibitor of vacuolar H⁺-ATPases (V-ATPases; K_i = 0.5 nM in N. crassa vacuolar membranes) and is greater than 1,000-fold selective for V-ATPases over Na⁺/K⁺-, Ca²⁺-, and H⁺-ATPases. Bafilomycin A₁ (100 nM) inhibits autophagosome maturation and protein degradation in H-4-II-E cells. It inhibits chloroquine-induced apoptosis in primary cerebellar granule neurons (CGNs) but not chloroquine-induced inhibition of macroautophagy. Bafilomycin A₁ (100 nM) reduces viral yield in the culture supernatant of Vero E6 and Huh7 cells, as well as HEK293T cells expressing human angiotensin-converting enzyme 2 (ACE2), infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). It also reduces lung RNA copy numbers and viral pneumonia in ACE2 transgenic mice infected with SARS-CoV-2 when administered at a dose of 0.1 mg/kg.

Bafilomycin A1 is a macrolide antibiotic. Bafilomycin A1 acts as a potent and selective inhibitor of vacuolar-type H+-ATPase.

Desiccate at -20°C, protect from light

1) Werner?et al.? (1984) Metabolic products of microorganisms. Bafilomycins, a new group of macrolide antibiotics. Production, isolation, chemical structure and biological activity; J. Antibiot.,?37?110 2) Drose and Altendorf? (1997)?Bafilomycins and concanamycins as inhibitors of V-ATPase and P-ATPase;?J. Exp. Biol.,?200?1 3) Yamamoto?et al. (1998)?Bafilomycin A1 prevents maturation of autophagic vacuoles by inhibiting fusion between autophagosomes and lysosomes in rat hepatoma cell line, H-4-II-E cells;?Cell Struct. Func.,?23?33