1-NM-PP1

1-NM-PP1 is a cell permeable inhibitor of kinases that have been mutated, by a single base substitution, to become ‘analog sensitive’ (as), as compared to the wild-type kinase. 1-NM-PP1 was first developed to optimally inhibit v-Src-as1, with an I338G substitution, preferentially over v-Src (IC50 = 4.2 nM versus 28 ?M, respectively).{17286} The homologous mutation in other kinases generated similar analog sensitivity (e.g., IC50 = 3.2 nM for c-Fyn-as1 versus 1.0 ?M for c-Fyn; 5.0 nM for Cdk2-as1 versus 29 ?M for Cdk2; 8.0 nM for CAMKII-as1 versus 24 ?M for CAMKII).{17287} This approach has been used to elucidate functions of several kinases in both mammalian and yeast systems.{17287,17288,17289,17290,17291}