General Description
A broad-based, cell-permeable, reversible, ATP-competitive serine-threonine kinase inhibitor. Potent inhibitor of myosin light chain kinase (K
i = 97 μM), protein kinase A (K
i = 3.0 μM), protein kinase C (K
i = 6 μM), and protein kinase G (K
i = 5.8 μM). Induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells. Also inhibits telomerase activity in quercetin-, H-89-, or herbimycin A-treated NPC-076 cells.
Biochem/physiol Actions
Target Ki: 3.0 μM, 97 μM, 6.0 μM, 5.8 μM against protein kinase A , myosin light chain kinase, protein kinase C , and protein kinase G, respectively