Table 3. . Protein kinase C inhibitors.
No. | Structure | Inhibitor class | Publication year | Activity |
---|---|---|---|---|
27 | ![]() |
Natural inhibitor (Staurosporine) | 1977, first isolated; 1986, the inhibitory activity against PKC was revealed | PKC (IC50 = 2.7 nM) |
28 | ![]() |
Semisynthetic (K-252 a) | 1986 | IC50 = 18–25 nM |
29 | ![]() |
Semisynthetic (K-252b) | 1986 | IC50 = 20 nM |
30 | ![]() |
Semisynthetic, 7-oxo Staurosporine (RK –1409) | 1992 | IC50 ≈ 1 nM |
31 | ![]() |
Natural (Calphostin C) | 1989 | IC50 = 0.05 µM |
32 | ![]() |
Synthetic (AEB071) | 2009 | PKC-α (IC50 = 2.1 nM) PKC-ϵ (IC50 = 6.1 nM) |
33 | ![]() |
Synthetic | 2011 | PKC-α (IC50 = 829 nM) PKC-ϵ (IC50 = 5 nM) |
34 | ![]() |
Synthetic | 2011 | PKC-βII (Ki = 29 nM) |
35 | ![]() |
Flosequinan-selective PKC inhibitor | 1992 | – |
36 | ![]() |
Ruboxistaurin | 2006 | PKC-βI (IC50 = 4.7 nM) PKC-βII (IC50 = 5.9 nM) |
PKC: Protein kinase C