| S2791 |
Sotrastaurin (AEB071) |
Sotrastaurin (AEB071) is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay; inactive to PKCζ. Phase 2. |
Pan |
PKCα, Ki: 0.95 nM |
| S1421 |
Staurosporine (STS) |
Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3. |
Pan |
PKCα, IC50: 2 nM |
| S7119 |
Go6976 |
Go6976 (PD406976) 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 |
PKCα, IC50: 2.3 nM |
| S7207 |
Bisindolylmaleimide IX (Ro 31-8220 Mesylate) |
Bisindolylmaleimide IX (Ro 31-8220 Mesylate) 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 |
PKCα, IC50: 5 nM |
| S2911 |
Go 6983 |
Go 6983 (GOE 6983, Gö 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 |
PKCα, IC50: 7 nM |
| S7208 |
Bisindolylmaleimide I (GF109203X) |
Bisindolylmaleimide I (GF109203X, GO 6850) is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor. |
Pan |
PKCα, IC50: 20 nM |
| S8064 |
Midostaurin |
Midostaurin is a multi-targeted kinase inhibitor, including PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50 ranging from 80-500 nM. |
Pan |
PKCα, IC50: 22 nM |
| S1055 |
Enzastaurin |
Enzastaurin is a potent PKCβ selective inhibitor with IC50 of 6 nM in cell-free assays, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3. |
Pan |
PKCα, IC50: 39 nM |
| S7663 |
Ruboxistaurin (LY333531) HCl |
Ruboxistaurin (LY333531) HCl is a β-specific protein kinase C inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively. |
Pan |
PKCα, IC50: 0.36 μM |
| S7862 |
Rottlerin |
Rottlerin (Mallotoxin, NSC 56346, NSC 94525), a natural compound purified from Mallotus Philippinensis, is a specific Protein kinase inhibitor with IC50 of 3 μM, 6 μM and 5.3 μM for PKCδ(from baculovirus-infected Sf9 insect cells), PKCδ(from porcine spleen) and CaM kinase III, respectively. Rottlerin also inhibits PKCα, PKCγ, PKCβ, PKCη, CKII and PKA with IC50 of 30 μM, 40 μM, 42 μM, 82 μM, 30 μM and 78 μM, respectively. |
Pan |
PKCα, IC50: 30 μM |
| S2327 |
Myricitrin |
Myricitrin (Myricitrine), a flavonoid compound isolated from the root bark of Myrica cerifera, which exerts antinociceptive effects. |
Pan |
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