Probe
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Information
ATP5F1B
Inhibitor
In Vitro Validations
Uniprot ID: P06576
Target Class:
Enzyme
Target SubClass: --
Potency: IC50
Potency Value: 20nM
Potency Assay: Enzyme-coupled ATPase assay.
The assay buffer consisted of 60 mM Tris–acetate pH 7.8, 1 mM MgCl2, 2.5 mM phosphoenolpyruvate and 1 mM KCN. The working solution was prepared at 2× for a final concertation of 0.4 mM NADH; 3 U ml−1 of pyruvate kinase + 4.5 U ml−1 lactate dehydrogenase (Sigma P0294); ± 10 μM FCCP. Unless otherwise specified, ATP was added as a 4× solution at 200 μM. Absorbance was monitored at 340 nm using a SpectraMax Plus 384 plate reader (Molecular Devices) set at 25 °C using Softmax Pro v.4.3 acquisition software. Fifty microliters of enzyme [purified yeast FoF1 ATP synthase] was added to 100 μl of working solution and monitored for 2 min, 50 μl of ATP was then added for a final volume of 200 μl and absorbance was monitored over 10 min.
PDB ID for probe-target interaction (3D structure):
7MD2
Target aliases:
ATP synthase subunit beta, mitochondrial, ATPSB, A ...
Target selectivity data for apoptolidin. ATP synthase resistance mutations in ATP5B or ATP5C eliminate both binding and cytotoxicity, providing evidence against off-target effects that contribute to cytotoxicity < 1 uM
