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Figure 2.
Figure 2. Kinetic analysis of the inhibition of IRK by
bisubstrate analog compound 2. a, E/V versus 1/ATP in the
presence of varying concentrations of compound 2. b, E/V versus
1/IRS727 in the presence of varying compound 2. For (a), the
apparent K[i] (compound 2) was 550  80
nM; for (b), the apparent K[i] (compound 2) was 750 90
nM. c, Product/Enzyme versus Time. This experiment monitors the
phosphopeptide (product) formation after a rapid dilution of the
enzyme -inhibitor complex to indirectly measure the k[off] for
dissociation of compound 2 from IRK; k[off] = 0.013 0.001
s-1.
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