Inhibitor of protein kinase C (IC 50 = 2.45 μ M) that displays ~ 10-fold selectivity over protein kinase A (IC 50 = 25.7 μ M). Also inhibits β -lactamase, malate dehydrogenase and chymotrypsin (IC 50 values are 8, 8 and 10 μ M respectively). Exhibits antiviral activity against GCV-sensitive and -resistant strains of human cytomegalovirus (HCMV) (IC 50 values range from 0.13-0.32 μ M). Shows no activity against herpes simplex virus (HSV).
1. fabre s, prudhomme m, rapp m. protein kinase c inhibitors; structure-activity relationships in k252c-related compounds. bioorg med chem 1993,1:193-196.2. hashimoto s. k-252a, a potent protein kinase inhibitor, blocks nerve growth factor-induced neurite outgrowth and changes in the phosphorylation of proteins in pc12h cells. j cell biol 1988,107:1531-1539.3. raychaudhuri sp, sanyal m, weltman h, kundu-raychaudhuri s. k252a, a high-affinity nerve growth factor receptor blocker, improves psoriasis: an in vivo study using the severe combined immunodeficient mouse-human skin model. j invest dermatol 2004,122:812-819.
