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 μM, respectively). The homologous mutation in other kinases generated similar analog sensitivity (e.g., IC50 = 3.2 nM for c-Fyn-as1 versus 1.0 μM for c-Fyn; 5.0 nM for Cdk2-as1 versus 29 μM for Cdk2; 8.0 nM for CAMKII-as1 versus 24 μM for CAMKII). This approach has been used to elucidate functions of several kinases in both mammalian and yeast systems.
A highly potent (IC50=4.3 nM) and uniquely specific tyrosine kinase inhibitor of a rationally engineered v-Src tyrosine kinase
ChEBI: 1-NM-PP1 is a pyrazolopyrimidine. It has a role as a tyrosine kinase inhibitor.
[1] bishop ac1, ubersax ja, petsch dt, matheos dp, gray ns, blethrow j, shimizu e, tsien jz, schultz pg, rose md, wood jl, morgan do, shokat km. a chemical switch for inhibitor-sensitive alleles of any protein kinase. nature. 2000 sep 21; 407 (6802): 395-401.
