Inhibitory profiling of S-014-1049 against mutant SK
Comparative study of the kinase activity of the 3 mutants
(CD15:SK, SBD34:SK, and
LD117:SK) of SK using ADP-Glo kinase assay and wild
type MTSK was used as a control. Significant inhibition of enzyme
activity was observed in SBD34:SK,
LD117:SK and MTSK compared to
CD15:SK. Hence, it can be inferred that the binding of
the compound with the protein, occurs in case of intact CD which
influences in the decrease of enzyme activity (Figure 2E).