UCN-1028c Light brown lyophilized solid. PROTECT FROM LIGHT. A cell permeable, highly specific inhibitor of protein kinase C (IC50 = 50 nM) that interacts with the protein’s regulatory domain by competing at the binding site of diacylglycerol and phorbol esters. Does not compete with Ca2+ or phospholipids. At higher concentrations inhibits myosin light chain kinase (IC50 > 5 µM), protein kinase A (IC50 > 50 µM), protein kinase G (IC50 > 25 µM), and p60v-src (IC50 > 50 µM). Induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells. Requires brief exposure to light for activation. Purity: ≥95% by HPLC. CAS 121263-19-2. Ref.: Jarvis, W.D., et al. 1994. Cancer Res. 54, 1707. Svetlov, S., and Nigami, S. 1993. Biochim. Biophys. Acta 1177, 75. Gopalakrishna, R., et al. 1992. FEBS Lett. 314, 149. Shimamato, H., et al. 1992. Br. J. Pharmacol. 107, 282. Bruns, R.F., et al. 1991. Biochem. Biophys. Res. Commun. 176, 288. Tamaoki, T., et al. 1990. Biotechnology 8, 732. Kobayashi, E., et al. 1989. Biochem. Biophys. Res. Commun. 159, 548. |
