1-nm-pp1

Description: 1-NM-PP1, a C3-modified analog of PP1, is a novel, potent and cell permeable protein kinase D (PKD) inhibitor with an IC50 of 0.398 uM. 1-NM-PP1 has shown the selective inhibition of protein kinases that have been mutated with the IC50 values of 28 uM, 1.0 uM, 3.4 uM, 29 uM, 24 uM, 4.3 nM, 3.2 nM, 120 nM, 5 nM and 8 nM for v-Src, c-Fyn, c-Abl, CDK2, CAMKII, v-Src-as1, c-Fyn-as1, cAbl-as2, CDK2-as1 and CAMKII-as1, respectively. 1-NM-PP1 inhibited each of the five target kinases at low nanomolar concentrations with target-specificities ranging from 85-fold to 400-fold measured against the most inhibitable wild-type kinases. In addition, the in vitro study has also revealed that Cdc28-as1 is highly sensitive to 1-NM-PP1 with ATP kinetic Km values of 35 uM and 322 uM, the Kcat values of 132 min-1 and 21.3 min-1, the Kcat/Km values of 3.7 and 0.066, the IC50 values of 22 uM and 0.002 uM for Cdc28/Clb2 and Cdc28-as1/Clb2, respectively

References: Nature. 2000 Sep 21; 407(6802):395-401.