| S2791 |
Sotrastaurin |
Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM; inactive to PKCζ. Phase 2. |
Pan |
PKCβ1, Ki: 0.64 nM |
| S1055 |
Enzastaurin (LY317615) |
Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3. |
Pan |
PKCβ, IC50: 6 nM |
| S7119 |
Go6976 |
Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
|
Pan |
PKCβ1, IC50: 6.2 nM |
| S2911 |
Go 6983 |
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ. |
Pan |
PKCβ, IC50: 7 nM |
| S7207 |
Ro 31-8220 Mesylate |
Ro 31-8220 is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively, and also shows potent inhibition against MAPKAP-K1b, MSK1, GSK3β and S6K1. |
Pan |
PKCβ2, IC50: 14 nM; PKCβ1, IC50: 24 nM |
| S7208 |
GF109203X |
GF109203X is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor. |
Pan |
PKCβ2, IC50: 16 nM; PKCβ1, IC50: 17 nM |