Enzastaurin (LY317615)

Pan PKC Inhibitor

Sotrastaurin : Pan-PKC inhibitor, PKCα, Ki=0.95 nM; PKCβ, Ki=0.64 nM; PKCδ, Ki=2.1 nM; PKCε, Ki=3.2 nM; PKCη, Ki=1.8 nM; PKCθ, Ki=0.22 nM.

Most Potent PKC Inhibitor

Go 6983 : PKCα, IC50=7 nM; PKCβ, IC50=7 nM; PKCγ, IC50=6 nM; PKCδ, IC50=10 nM.

PKC Inhibitor in Clinical Trial

Dequalinium Chloride : Phase III for Bacterial Vaginosis.

Newest PKC Inhibitor

Ro 31-8220 Mesylate ^New : 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.

SD-208 ^New

SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.

LDN-214117 ^New

LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.

Staurosporine

Staurosporine 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.

Sotrastaurin

Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with K_i of 0.22 nM in a cell-free assay; inactive to PKCζ. Phase 2.

Features:Unlike former PKC inhibitors, Sotrastaurin does not enhance apoptosis of murine T-cell blasts in a model of activation-induced cell death.

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.

Bisindolylmaleimide I (GF109203X)

Bisindolylmaleimide I (GF109203X) 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.

Features:Greater selectivity than PKC inhibitor staurosporine. GF109203X is a chemical probe for studying PKC signal transduction pathways. Potential for use in a variety of cancers.

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.

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.

Dequalinium Chloride

Dequalinium Chloride is a PKC inhibitor with IC50 of 7-18 μM, and also a selective blocker of apamin-sensitive K+ channels with IC50 of 1.1 μM.