PKC

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

PKC Products

All (20) PKC Inhibitors (17) PKC Activators (3) New PKC Products

Catalog No.	Information	Product Use Citations	Product Validations
S1055	Enzastaurin (LY317615) Enzastaurin (LY317615) 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.	Mol Carcinog, 2020, 59(1):87-103 Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193	The protein kinase C (PKC)–specific inhibitor enzastaurin induces apoptosis of lupus B cells and prevents lupus development in Sle mice. C, Levels of serum IgG anti–double-stranded DNA (anti-dsDNA) and antihistone/anti-dsDNA autoantibodies from vehicle-treated control mice and enzastaurin-treated mice, as analyzed by enzyme-linked immunosorbent assay. Bars in A–C show the mean SD of 3 independent experiments. D, Representative immunofluorescent images of IgG deposition (top) and glomeruli (bottom) in kidney sections from Sle1.Sle3 mice treated with vehicle or enzastaurin. Original magnification 20 (top); 40 (bottom). PAS periodic acid–Schiff.
S2791	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.	Mol Carcinog, 2020, 59(1):87-103 Exp Cell Res, 2020, 386(2):111735 Nat Cell Biol, 2019, 21(6):778-790	Lysates from H3122 and MGH006 cells treated with 1 µM PMA in the presence or absence of 0.3 µM sotrastaurin (SOT) were fractionated. Immunoblotting was performed with the indicated antibodies.
S1421	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.	Cancer Discov, 2019, 10.1158/2159-8290.CD-19-0270 Autophagy, 2019, 10.1080/15548627 Autophagy, 2019, 15(2):295-311
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.	Nat Cell Biol, 2019, 21(6):778-790 Nat Commun, 2019, 10(1):4836 Nat Commun, 2019, 10(1):2924	(a) In vitro kinase reactions were performed by using GSTp531-64 (FP267) as substrate and GST-CK1δ (FP449) as enzyme, or using (b) GST-CK1δ375–428 (FP1183) as substrate and recombinant PKCα as enzyme in combination with one of three PKC-specific inhibitors (Go-6983, enzastaurin, and bisindolylmaleimide I (BIM I), respectively). Data are presented as normalized bar graph.
S7208	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.	Cancer Cell Int, 2019, 19:241 Front Physiol, 2019, 10:167 Onco Targets Ther, 2019, 12:1137-1146	Effect of PKC inhibitor on DHPG-stimulated Cx43 and ERK1/2 phosphorylation response and GJIC inhibition. Cells were treated with the PKC inhibitor GF109203X (different concentrations indicated) for 30 min prior to DHPG (100 lM, 15 min) treatment. a Representative immunoblots with an anti-Cx43 antibody are shown. b Representative immunoblots with a phospho-specific antibody recognizing the dually phosphorylated form of ERK1/2 (Thr202/Tyr204) and an antibody recognizing total ERK1/2 are shown. Quantitative analysis of the Cx43-P2/Cx43-P0?1 ratio and the phospho-ERK1/2 (p-ERK1/2)/total-ERK1/2 (t-ERK1/2) ratio are shown below the representative immunoblots, respectively. C Cells were incubated without (a) or with 100 lM DHPG (b) or with 100 μM DHPG in combination with 10 μM GF109203X (c) and scrape loaded (9100). d Cells were exposed to GF109203X (different concentrations indicated) alone (filled square) or 100 μM DHPG and GF109203X (filled diamond) prior to measurement of GJIC by scrape loading. Data are shown as mean ± SEM for three separate experiments performed in triplicate (*p<0.05 vs. NC, n = 3, +GF109203X for 0.1, 1, 5 or 10 μM)
S6723^New	LXS-196 LXS-196 is a selective inhibitor of protein kinase C (PKC).
S6577^New	PKC-theta inhibitor PKC-theta inhibitor inhibits PKC-θ with an IC50 of 12 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.	Sci Transl Med, 2019, 9(415) Int J Biochem Cell Biol, 2019, 110:111-121 Free Radic Res, 2019, 53(3):348-358
S2554	Daphnetin Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities.	Int Immunopharmacol, 2019, 72:195-203 Inflamm Res, 2017, 66(7):579-589	C57/BL6 mice (5 mice/group) were intraperitoneally injected with daphnetin (DFN, 5 mg/kg) or DMSO, and then challenged with LPS (37.5 mg/kg) or saline. 16 h after LPS challenge, mice were sacrificed, and then lung and serum were collected. c, Representative photomicrographs showed H&E staining of lung tissue.
S4066	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.
S1292	Chelerythrine Chloride Chelerythrine is a potent, selective antagonist of PKC with IC50 of 0.66 μM.
S2391	Quercetin Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Phase 4.	Front Cell Neurosci, 2019, 13:316 NPJ Precis Oncol, 2019, 3:16 Clin Cancer Res, 2018, 10.1158/1078-0432	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
S3661	2-Methoxy-1,4-naphthoquinone 2-Methoxy-1,4-naphthoquinone, isolated from the leaves of Impatiens glandulifera, specifically suppressed the expression of PKC βI, δ, and ζ in a concentration-dependent manner in Raji cells.
S2327	Myricitrin Myricitrin, a flavonoid compound isolated from the root bark of Myrica cerifera, which exerts antinociceptive effects.
S7663	Ruboxistaurin HCl(LY333531 ) LY333531 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.	J Clin Invest, 2019, 10.1172/JCI130730 PLoS One, 2019, 14(3):e0211309 Cardiovasc Pathol, 2019, 41:11-17
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.	Oncogene, 2019, 38(1):120-139 EBioMedicine, 2019, 40:151-162 Acta Physiol, 2018, 223(3):e13055	Erk5 activation depends on Mek5, classical PKC and Mek1/2. MOVAS cells were serum-starved overnight and then treated for 1 h if not indicated otherwise with inhibitors targeting Jnk (SP600125, 10 μM), p38 (SB203580, 10 μM), Mek1/2 (CI-1040, 3 μM), Jak2 (AG490, 10 μM), Src (SU6656, 0.5 μM), Go6983 (PKC, 1 μM), Gö6976 (classical PKC, 1 μM), proteasomes (MG132, 25 μM), TPA (100 ng/ml for 15 min to activate PKCs or overnight to inhibit) and Mek5 (BIX02189, 1 μM), as well as Ca2 + chelators (EDTA, 2 mM; BAPTA-AM, 10 μM; both with 30 min preincubation), followed by stimulation with 20 ng/ml PDGF-BB for 10 min. Total cell lysates (TCL) were prepared and subjected to SDS-PAGE. Erk5 and PDGFRβ activities were measured by band shift and Tyr857 phosphorylation, respectively, using immunoblotting. Panel E and G show representative immunoblots.
S8064	Midostaurin (PKC412) Midostaurin (pkc412) 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.	Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0832 Cancer Res, 2019, 10.1158/0008-5472 Cancer Lett, 2019, 445:34-44	(f and g) Induction of apoptosis in HMC-1.1 and -1.2, respectively. Columns represent the mean of three independent experiments and the bars represent the standard error. ctrl, control; mido, midostaurin.
S7791^New	Phorbol 12-myristate 13-acetate (PMA) Phorbol 12-myristate 13-acetate (PMA), a potent activator of PKC, is active at nanomolar concentrations.	Oncogenesis, 2018, 7(11):91 Clin Exp Immunol, 2016, 184(2):147-58
S3819	Decursinol angelate Decursinol angelate is a cytotoxic and protein kinase C activating agent from the root of Angelica gigas.
s9101	Ingenol Ingenol, a plant-derived diterpenoid, is a weak PKC activator and possesses important anticancer activity.

Catalog No.	Information	Product Use Citations	Product Validations
S1055	Enzastaurin (LY317615) Enzastaurin (LY317615) 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.	Mol Carcinog, 2020, 59(1):87-103 Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193	The protein kinase C (PKC)–specific inhibitor enzastaurin induces apoptosis of lupus B cells and prevents lupus development in Sle mice. C, Levels of serum IgG anti–double-stranded DNA (anti-dsDNA) and antihistone/anti-dsDNA autoantibodies from vehicle-treated control mice and enzastaurin-treated mice, as analyzed by enzyme-linked immunosorbent assay. Bars in A–C show the mean SD of 3 independent experiments. D, Representative immunofluorescent images of IgG deposition (top) and glomeruli (bottom) in kidney sections from Sle1.Sle3 mice treated with vehicle or enzastaurin. Original magnification 20 (top); 40 (bottom). PAS periodic acid–Schiff.
S2791	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.	Mol Carcinog, 2020, 59(1):87-103 Exp Cell Res, 2020, 386(2):111735 Nat Cell Biol, 2019, 21(6):778-790	Lysates from H3122 and MGH006 cells treated with 1 µM PMA in the presence or absence of 0.3 µM sotrastaurin (SOT) were fractionated. Immunoblotting was performed with the indicated antibodies.
S1421	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.	Cancer Discov, 2019, 10.1158/2159-8290.CD-19-0270 Autophagy, 2019, 10.1080/15548627 Autophagy, 2019, 15(2):295-311
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.	Nat Cell Biol, 2019, 21(6):778-790 Nat Commun, 2019, 10(1):4836 Nat Commun, 2019, 10(1):2924	(a) In vitro kinase reactions were performed by using GSTp531-64 (FP267) as substrate and GST-CK1δ (FP449) as enzyme, or using (b) GST-CK1δ375–428 (FP1183) as substrate and recombinant PKCα as enzyme in combination with one of three PKC-specific inhibitors (Go-6983, enzastaurin, and bisindolylmaleimide I (BIM I), respectively). Data are presented as normalized bar graph.
S7208	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.	Cancer Cell Int, 2019, 19:241 Front Physiol, 2019, 10:167 Onco Targets Ther, 2019, 12:1137-1146	Effect of PKC inhibitor on DHPG-stimulated Cx43 and ERK1/2 phosphorylation response and GJIC inhibition. Cells were treated with the PKC inhibitor GF109203X (different concentrations indicated) for 30 min prior to DHPG (100 lM, 15 min) treatment. a Representative immunoblots with an anti-Cx43 antibody are shown. b Representative immunoblots with a phospho-specific antibody recognizing the dually phosphorylated form of ERK1/2 (Thr202/Tyr204) and an antibody recognizing total ERK1/2 are shown. Quantitative analysis of the Cx43-P2/Cx43-P0?1 ratio and the phospho-ERK1/2 (p-ERK1/2)/total-ERK1/2 (t-ERK1/2) ratio are shown below the representative immunoblots, respectively. C Cells were incubated without (a) or with 100 lM DHPG (b) or with 100 μM DHPG in combination with 10 μM GF109203X (c) and scrape loaded (9100). d Cells were exposed to GF109203X (different concentrations indicated) alone (filled square) or 100 μM DHPG and GF109203X (filled diamond) prior to measurement of GJIC by scrape loading. Data are shown as mean ± SEM for three separate experiments performed in triplicate (*p<0.05 vs. NC, n = 3, +GF109203X for 0.1, 1, 5 or 10 μM)
S6723^New	LXS-196 LXS-196 is a selective inhibitor of protein kinase C (PKC).
S6577^New	PKC-theta inhibitor PKC-theta inhibitor inhibits PKC-θ with an IC50 of 12 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.	Sci Transl Med, 2019, 9(415) Int J Biochem Cell Biol, 2019, 110:111-121 Free Radic Res, 2019, 53(3):348-358
S2554	Daphnetin Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities.	Int Immunopharmacol, 2019, 72:195-203 Inflamm Res, 2017, 66(7):579-589	C57/BL6 mice (5 mice/group) were intraperitoneally injected with daphnetin (DFN, 5 mg/kg) or DMSO, and then challenged with LPS (37.5 mg/kg) or saline. 16 h after LPS challenge, mice were sacrificed, and then lung and serum were collected. c, Representative photomicrographs showed H&E staining of lung tissue.
S4066	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.
S1292	Chelerythrine Chloride Chelerythrine is a potent, selective antagonist of PKC with IC50 of 0.66 μM.
S2391	Quercetin Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Phase 4.	Front Cell Neurosci, 2019, 13:316 NPJ Precis Oncol, 2019, 3:16 Clin Cancer Res, 2018, 10.1158/1078-0432	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
S3661	2-Methoxy-1,4-naphthoquinone 2-Methoxy-1,4-naphthoquinone, isolated from the leaves of Impatiens glandulifera, specifically suppressed the expression of PKC βI, δ, and ζ in a concentration-dependent manner in Raji cells.
S2327	Myricitrin Myricitrin, a flavonoid compound isolated from the root bark of Myrica cerifera, which exerts antinociceptive effects.
S7663	Ruboxistaurin HCl(LY333531 ) LY333531 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.	J Clin Invest, 2019, 10.1172/JCI130730 PLoS One, 2019, 14(3):e0211309 Cardiovasc Pathol, 2019, 41:11-17
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.	Oncogene, 2019, 38(1):120-139 EBioMedicine, 2019, 40:151-162 Acta Physiol, 2018, 223(3):e13055	Erk5 activation depends on Mek5, classical PKC and Mek1/2. MOVAS cells were serum-starved overnight and then treated for 1 h if not indicated otherwise with inhibitors targeting Jnk (SP600125, 10 μM), p38 (SB203580, 10 μM), Mek1/2 (CI-1040, 3 μM), Jak2 (AG490, 10 μM), Src (SU6656, 0.5 μM), Go6983 (PKC, 1 μM), Gö6976 (classical PKC, 1 μM), proteasomes (MG132, 25 μM), TPA (100 ng/ml for 15 min to activate PKCs or overnight to inhibit) and Mek5 (BIX02189, 1 μM), as well as Ca2 + chelators (EDTA, 2 mM; BAPTA-AM, 10 μM; both with 30 min preincubation), followed by stimulation with 20 ng/ml PDGF-BB for 10 min. Total cell lysates (TCL) were prepared and subjected to SDS-PAGE. Erk5 and PDGFRβ activities were measured by band shift and Tyr857 phosphorylation, respectively, using immunoblotting. Panel E and G show representative immunoblots.
S8064	Midostaurin (PKC412) Midostaurin (pkc412) 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.	Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0832 Cancer Res, 2019, 10.1158/0008-5472 Cancer Lett, 2019, 445:34-44	(f and g) Induction of apoptosis in HMC-1.1 and -1.2, respectively. Columns represent the mean of three independent experiments and the bars represent the standard error. ctrl, control; mido, midostaurin.

Catalog No.	Information	Product Use Citations
S7791^New	Phorbol 12-myristate 13-acetate (PMA) Phorbol 12-myristate 13-acetate (PMA), a potent activator of PKC, is active at nanomolar concentrations.	Oncogenesis, 2018, 7(11):91 Clin Exp Immunol, 2016, 184(2):147-58
S3819	Decursinol angelate Decursinol angelate is a cytotoxic and protein kinase C activating agent from the root of Angelica gigas.
s9101	Ingenol Ingenol, a plant-derived diterpenoid, is a weak PKC activator and possesses important anticancer activity.

Catalog No.

Information

Product Use Citations

Product Validations

S7791^New