Light yellow to yellow solid. Naturally-occurring alkaloid. Potent, selective, and cell-permeable inhibitor of protein kinase C (IC₅₀ = 660 nM). Acts on the catalytic domain of PKC. A competitive inhibitor with respect to the phosphate acceptor and a non-competitive inhibitor with respect to ATP. Over ten-fold more potent than H-7, HCl (Cat. No. 371955). Inhibits thromboxane formation and phosphoinositide metabolism in platelets. Also induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells. Purity: ≥97% by NMR. RTECS FL9200000, CAS 3895-92-9.

Merck Index: 14, 2051
Ref.: Kandasamy, R.A., et al. 1995. J. Biol. Chem. 270 29209. Jarvis, W.D., et al. 1994. Cancer Res. 54, 1707. Barg, J., et al. 1992. J. Neurochem. 59, 1145. Herbert, J.M., et al. 1990. Biochem. Biophys. Res. Commun. 172, 993. Ko, F., et al. 1990. Biochim. Biophys. Acta 1052, 360. Walterova, D., et al. J. Med. Chem. 24, 1100.
R: 20/21/22-36/37/38; S: 26-36