TABLE 1

Enzymatic formation rates of R-361015 from R-361015-SG in human liver microsomes and human liver cytosols and in the presence of human glutaredoxin

R-361015-SG (1 μM) was incubated for 2.5 min in human liver microsomes (0.01 mg/ml protein) or human liver cytosols (0.01 mg/ml protein) or with recombinant human glutaredoxin (0.0336 μg/ml) in the presence of 5 mM GSH. R-361015 formed in buffer containing 5 mM GSH was ascribed to nonenzymatic background.