Bafilomycin A1

Bafilomycin A1 is a bacterial metabolite that has been found in Streptomyces and has diverse biological activities. It is an inhibitor of vacuolar H+-ATPases (V-ATPases, Ki = 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.Formal Name: (3Z,5E,7R,8S,9S,11E,13E,15S,16R)-8-hydroxy-16-[(1S,2R,3S)-2-hydroxy-1-methyl-3-[(2R,4R,5S,6R)-tetrahydro-2,4-dihydroxy-5-methyl-6-(1-methylethyl)-2H-pyran-2-yl]butyl]-3,15-dimethoxy-5,7,9,11-tetramethyl-oxacyclohexadeca-3,5,11,13-tetraen-2-one. CAS Number: 88899-55-2. Synonyms: NSC 381866. Molecular Formula: C35H58O9. Formula Weight: 622.8. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 5 mg/ml, Methanol: 5 mg/ml. lambdamax: 248, 288 nm. SMILES: C[C@H]([C@@](C[C@H]1O)(O[C@H](C(C)C)[C@H]1C)O)[C@H](O)[C@@H]([C@](OC(/C(OC)=C/C(C)=C/[C@@H](C)[C@@H](O)[C@@H](C)C2)=O)([H])[C@H](/C=C/C=C2\C)OC)C. InChi Code: InChI=1S/C35H58O9/c1-19(2)32-24(7)27(36)18-35(40,44-32)26(9)31(38)25(8)33-28(41-10)14-12-13-20(3)15-22(5)30(37)23(6)16-21(4)17-29(42-11)34(39)43-33/h12-14,16-17,19,22-28,30-33,36-38,40H,15,18H2,1-11H3/b14-12+,20-13+,21-16+,29-17-/t22-,23+,24-,25-,26-. InChi Key: XDHNQDDQEHDUTM-JQWOJBOSSA-N. Origin: Bacterium/Streptomyces sp..