PKC

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PKC Signaling Pathway Map

PKC Signaling Pathways

PKC Products

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  • New PKC Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0010New Hypocrellin A Hypocrellin A (HA) is a perylenequinone isolated from Shiraia bambusicola that shows antiviral, antimicrobial and anticancer activity through mediating multiple signaling pathways. Hypocrellin A also is a selective and potent inhibitor of PKC.
S0069 VTX-27 VTX-27 (Compound 27) is a potent and selective inhibitor of protein kinase C θ (PKC θ) with Ki of 0.08 nM and 16 nM for PKC θ and PKC δ, respectively.
Elife, 2021, 10e68473
S0754 Bisindolylmaleimide IV Bisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) is a potent inhibitor of protein kinase C (PKC) with IC50 of 0.55 μM. Bisindolylmaleimide IV also inhibits PKA with IC50 of 11.8μM. Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with IC50 of 0.2 μM.
Elife, 2021, 10e68473
S0780 Oncrasin-1 Oncrasin-1 (Onc-1) is a potent RNA polymerase II inhibitor with antitumor activity that kills various human lung cancer cells with K-Ras mutations. Oncrasin-1 drives abnormal aggregation of protein kinase C iota (PKCι) in nucleus of sensitive cells but not in resistant cells.
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.
Nat Cell Biol, 2022, 24(1):88-98
Oncogene, 2022, 10.1038/s41388-022-02179-z
Sci Rep, 2022, 12(1):7
S1113 GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
Mech Ageing Dev, 2022, 202:111633
Oncogene, 2021, 10.1038/s41388-021-01932-0
Breast Cancer Res, 2021, 23(1):81
S1292 Chelerythrine Chloride (NSC 646662) Chelerythrine Chloride (NSC 646662, Broussonpapyrine) is a potent, selective antagonist of PKC with IC50 of 0.66 μM.
Nutr Neurosci, 2022, 1-19
J Biol Chem, 2015, 290(34):20841-55
Peptides, 2015, 73:67-76
S1421 Staurosporine (AM-2282) Staurosporine (AM-2282, Antibiotic AM-2282, 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.
Cancer Res, 2022, canres.0218.2021
Neurotherapeutics, 2022, 10.1007/s13311-022-01212-z
Anal Chem, 2022, 10.1021/acs.analchem.1c05455
S1573 Fasudil (HA-1077) HCl Fasudil (HA-1077, AT-877), a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
Aging Cell, 2022, e13587
Cell Death Dis, 2022, 13(2):138
Sci Rep, 2022, 12(1):7
S2327 Myricitrin Myricitrin (Myricitrine), a flavonoid compound isolated from the root bark of Myrica cerifera, which exerts antinociceptive effects.
Molecules, 2021, 26(5)1210
S2391 Quercetin (NSC 9221) Quercetin (NSC 9221, Sophoretin, C.I. 75720), 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. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Mol Neurobiol, 2022, 10.1007/s12035-021-02712-3
Nucleic Acids Res, 2021, gkab538
S2485 Mitoxantrone (NSC-301739) 2HCl Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.
J Cell Biochem, 2022, 10.1002/jcb.30213
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancers (Basel), 2021, 13(8)1954
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.
Sci Rep, 2021, 11(1):11491
Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7
Int Immunopharmacol, 2019, 72:195-203
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.
Sci Rep, 2022, 12(1):7
Nat Commun, 2021, 12(1):2507
Nat Commun, 2021, 12(1):4566
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.
Nat Cell Biol, 2022, 24(1):88-98
Sci Rep, 2022, 12(1):7
Theranostics, 2021, 11(10):4728-4742
S2964 HA-100 dihydrochloride HA-100 dihydrochloride is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase with IC50 of 4 μM, 8 μM, 12 μM and 240 μM, respectively.
S3273 Hypericin Hypericin (Hyp, HY) is a naturally occurring substance found in the common St. John's Wort (Hypericum species) with antidepressive, antineoplastic and antiviral (human immunodeficiency and hepatitis C virus) activities. Hypericin has inhibitory effects on MAO (monoaminoxidase), PKC (protein kinase C), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450).
Eur J Pharmacol, 2021, 900:174071
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.
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.
Vet Microbiol, 2020, 251:108913
Neoplasia, 2020, 22(10):470-483
S6214New H-1152 dihydrochloride H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.
S6424 TAS-301 TAS-301 is an inhibitor of smooth muscle cell migration and proliferation. TAS-301 inhibits intimal thickening after balloon injury to rat carotid arteries, and inhibits PKC activation induced by PDGF.
S6577 PKC-theta inhibitor PKC-theta inhibitor (compound 20) inhibits PKC-θ with an IC50 of 18 nM.
Free Radic Biol Med, 2021, 174:40-56
bioRxiv, 2021, 10.1101/2021.05.07.442906
S6723 Darovasertib (LXS-196) Darovasertib (LXS-196, IDE-196) is a selective inhibitor of protein kinase C (PKC).
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.
Cell Chem Biol, 2021, S2451-9456(21)00303-2
Biochimie, 2021, 184:8-17
J Cell Physiol, 2020, 10.1002/jcp.30207
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 Rep, 2022, 12(1):7
Elife, 2021, 10e68473
Front Cell Dev Biol, 2021, 9:631163
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.
Sci Signal, 2022, 15(719):eabd0033
Sci Rep, 2022, 12(1):7
Hum Cell, 2022, 10.1007/s13577-022-00675-8
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.
ERJ Open Res, 2022, 8(2)00596-2021
Nat Commun, 2021, 12(1):3493
J Ethnopharmacol, 2021, 283:114674
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.
Food Funct, 2022, 10.1039/d1fo04198c
Biomed Pharmacother, 2022, 145:112437
bioRxiv, 2021, 10.1101/2021.05.07.442906
S8064 Midostaurin (PKC412) Midostaurin (pkc412, CGP 41251) 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.
Mol Cancer Ther, 2022, OF1-OF11
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3458
Leukemia, 2021, 10.1038/s41375-021-01308-z
S8388 ML-7 HCl ML-7 is an inhibitor of smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs. ML-7 also inhibits PKA and PKC with Ki of 21 μM and 42 μM, respectively.
Oxid Med Cell Longev, 2021, 2021:6620873
J Cell Sci, 2021, 134(1)jcs244616
Mol Cell Endocrinol, 2021, 535:111390
S9522 Valrubicin Valrubicin is a chemotherapy drug used to treat bladder cancer. Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively.
A5155 PKC epsilon Rabbit Recombinant mAb PKC epsilon Rabbit Recombinant mAb detects endogenous level of PKC epsilon.
A5215 PKC eta Rabbit Recombinant mAb PKC eta Rabbit Recombinant mAb detects endogenous level of total PKC eta.
S3289 Daphnoretin Daphnoretin (Dephnoretin, Thymelol), a biologically active compound isolated from Wikstroemia indica C.A. Mey., is a protein kinase C (PKC) activator. Daphnoretin inhibits the proliferation, invasion, and migration of tumor cells and promote its apoptosis by regulating the activity of Akt signal pathway.
S3819 Decursinol angelate Decursinol angelate is a cytotoxic and protein kinase C activating agent from the root of Angelica gigas.
S7791 Phorbol 12-myristate 13-acetate (PMA) Phorbol 12-myristate 13-acetate (PMA,12-O-Tetradecanoylphorbol-13-acetate, TPA, Phorbol myristate acetate), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P).
Cell Mol Immunol, 2022, 10.1038/s41423-022-00841-w
Oncogene, 2022, 10.1038/s41388-022-02197-x
Sci Rep, 2022, 12(1):1626
S9101 Ingenol Ingenol, a plant-derived diterpenoid, is a weak PKC activator and possesses important anticancer activity.
Sci Rep, 2020, 10(1):13124
E0124New Chelerythrine

Chelerythrine (Toddaline, Broussonpapyrine) is a potent, selective antagonist of PKC with an IC50 of 0.66 μM. Chelerythrine also inhibits the BclXL-Bak BH3 peptide binding with an IC50 of 1.5 μM. Chelerythrine shows antitumor, antidiabetic and anti-inflammatory activity.

Nutr Neurosci, 2022, 1-19
S2323 Methyl-Hesperidin Methyl Hesperidin is a flavanone glycoside (flavonoid) (C28H34O15) found abundantly in citrus fruits. Its aglycone form is called hesperetin.
E0010New Hypocrellin A Hypocrellin A (HA) is a perylenequinone isolated from Shiraia bambusicola that shows antiviral, antimicrobial and anticancer activity through mediating multiple signaling pathways. Hypocrellin A also is a selective and potent inhibitor of PKC.
S0069 VTX-27 VTX-27 (Compound 27) is a potent and selective inhibitor of protein kinase C θ (PKC θ) with Ki of 0.08 nM and 16 nM for PKC θ and PKC δ, respectively.
Elife, 2021, 10e68473
S0754 Bisindolylmaleimide IV Bisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) is a potent inhibitor of protein kinase C (PKC) with IC50 of 0.55 μM. Bisindolylmaleimide IV also inhibits PKA with IC50 of 11.8μM. Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with IC50 of 0.2 μM.
Elife, 2021, 10e68473
S0780 Oncrasin-1 Oncrasin-1 (Onc-1) is a potent RNA polymerase II inhibitor with antitumor activity that kills various human lung cancer cells with K-Ras mutations. Oncrasin-1 drives abnormal aggregation of protein kinase C iota (PKCι) in nucleus of sensitive cells but not in resistant cells.
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.
Nat Cell Biol, 2022, 24(1):88-98
Oncogene, 2022, 10.1038/s41388-022-02179-z
Sci Rep, 2022, 12(1):7
S1113 GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
Mech Ageing Dev, 2022, 202:111633
Oncogene, 2021, 10.1038/s41388-021-01932-0
Breast Cancer Res, 2021, 23(1):81
S1292 Chelerythrine Chloride (NSC 646662) Chelerythrine Chloride (NSC 646662, Broussonpapyrine) is a potent, selective antagonist of PKC with IC50 of 0.66 μM.
Nutr Neurosci, 2022, 1-19
J Biol Chem, 2015, 290(34):20841-55
Peptides, 2015, 73:67-76
S1421 Staurosporine (AM-2282) Staurosporine (AM-2282, Antibiotic AM-2282, 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.
Cancer Res, 2022, canres.0218.2021
Neurotherapeutics, 2022, 10.1007/s13311-022-01212-z
Anal Chem, 2022, 10.1021/acs.analchem.1c05455
S1573 Fasudil (HA-1077) HCl Fasudil (HA-1077, AT-877), a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
Aging Cell, 2022, e13587
Cell Death Dis, 2022, 13(2):138
Sci Rep, 2022, 12(1):7
S2327 Myricitrin Myricitrin (Myricitrine), a flavonoid compound isolated from the root bark of Myrica cerifera, which exerts antinociceptive effects.
Molecules, 2021, 26(5)1210
S2391 Quercetin (NSC 9221) Quercetin (NSC 9221, Sophoretin, C.I. 75720), 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. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Mol Neurobiol, 2022, 10.1007/s12035-021-02712-3
Nucleic Acids Res, 2021, gkab538
S2485 Mitoxantrone (NSC-301739) 2HCl Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.
J Cell Biochem, 2022, 10.1002/jcb.30213
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancers (Basel), 2021, 13(8)1954
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.
Sci Rep, 2021, 11(1):11491
Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7
Int Immunopharmacol, 2019, 72:195-203
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.
Sci Rep, 2022, 12(1):7
Nat Commun, 2021, 12(1):2507
Nat Commun, 2021, 12(1):4566
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.
Nat Cell Biol, 2022, 24(1):88-98
Sci Rep, 2022, 12(1):7
Theranostics, 2021, 11(10):4728-4742
S2964 HA-100 dihydrochloride HA-100 dihydrochloride is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase with IC50 of 4 μM, 8 μM, 12 μM and 240 μM, respectively.
S3273 Hypericin Hypericin (Hyp, HY) is a naturally occurring substance found in the common St. John's Wort (Hypericum species) with antidepressive, antineoplastic and antiviral (human immunodeficiency and hepatitis C virus) activities. Hypericin has inhibitory effects on MAO (monoaminoxidase), PKC (protein kinase C), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450).
Eur J Pharmacol, 2021, 900:174071
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.
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.
Vet Microbiol, 2020, 251:108913
Neoplasia, 2020, 22(10):470-483
S6214New H-1152 dihydrochloride H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.
S6424 TAS-301 TAS-301 is an inhibitor of smooth muscle cell migration and proliferation. TAS-301 inhibits intimal thickening after balloon injury to rat carotid arteries, and inhibits PKC activation induced by PDGF.
S6577 PKC-theta inhibitor PKC-theta inhibitor (compound 20) inhibits PKC-θ with an IC50 of 18 nM.
Free Radic Biol Med, 2021, 174:40-56
bioRxiv, 2021, 10.1101/2021.05.07.442906
S6723 Darovasertib (LXS-196) Darovasertib (LXS-196, IDE-196) is a selective inhibitor of protein kinase C (PKC).
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.
Cell Chem Biol, 2021, S2451-9456(21)00303-2
Biochimie, 2021, 184:8-17
J Cell Physiol, 2020, 10.1002/jcp.30207
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 Rep, 2022, 12(1):7
Elife, 2021, 10e68473
Front Cell Dev Biol, 2021, 9:631163
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.
Sci Signal, 2022, 15(719):eabd0033
Sci Rep, 2022, 12(1):7
Hum Cell, 2022, 10.1007/s13577-022-00675-8
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.
ERJ Open Res, 2022, 8(2)00596-2021
Nat Commun, 2021, 12(1):3493
J Ethnopharmacol, 2021, 283:114674
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.
Food Funct, 2022, 10.1039/d1fo04198c
Biomed Pharmacother, 2022, 145:112437
bioRxiv, 2021, 10.1101/2021.05.07.442906
S8064 Midostaurin (PKC412) Midostaurin (pkc412, CGP 41251) 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.
Mol Cancer Ther, 2022, OF1-OF11
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3458
Leukemia, 2021, 10.1038/s41375-021-01308-z
S8388 ML-7 HCl ML-7 is an inhibitor of smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs. ML-7 also inhibits PKA and PKC with Ki of 21 μM and 42 μM, respectively.
Oxid Med Cell Longev, 2021, 2021:6620873
J Cell Sci, 2021, 134(1)jcs244616
Mol Cell Endocrinol, 2021, 535:111390
S9522 Valrubicin Valrubicin is a chemotherapy drug used to treat bladder cancer. Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively.
A5155 PKC epsilon Rabbit Recombinant mAb PKC epsilon Rabbit Recombinant mAb detects endogenous level of PKC epsilon.
A5215 PKC eta Rabbit Recombinant mAb PKC eta Rabbit Recombinant mAb detects endogenous level of total PKC eta.
S3289 Daphnoretin Daphnoretin (Dephnoretin, Thymelol), a biologically active compound isolated from Wikstroemia indica C.A. Mey., is a protein kinase C (PKC) activator. Daphnoretin inhibits the proliferation, invasion, and migration of tumor cells and promote its apoptosis by regulating the activity of Akt signal pathway.
S3819 Decursinol angelate Decursinol angelate is a cytotoxic and protein kinase C activating agent from the root of Angelica gigas.
S7791 Phorbol 12-myristate 13-acetate (PMA) Phorbol 12-myristate 13-acetate (PMA,12-O-Tetradecanoylphorbol-13-acetate, TPA, Phorbol myristate acetate), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P).
Cell Mol Immunol, 2022, 10.1038/s41423-022-00841-w
Oncogene, 2022, 10.1038/s41388-022-02197-x
Sci Rep, 2022, 12(1):1626
S9101 Ingenol Ingenol, a plant-derived diterpenoid, is a weak PKC activator and possesses important anticancer activity.
Sci Rep, 2020, 10(1):13124
E0124New Chelerythrine

Chelerythrine (Toddaline, Broussonpapyrine) is a potent, selective antagonist of PKC with an IC50 of 0.66 μM. Chelerythrine also inhibits the BclXL-Bak BH3 peptide binding with an IC50 of 1.5 μM. Chelerythrine shows antitumor, antidiabetic and anti-inflammatory activity.

Nutr Neurosci, 2022, 1-19
E0010New Hypocrellin A Hypocrellin A (HA) is a perylenequinone isolated from Shiraia bambusicola that shows antiviral, antimicrobial and anticancer activity through mediating multiple signaling pathways. Hypocrellin A also is a selective and potent inhibitor of PKC.
S6214New H-1152 dihydrochloride H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.
E0124New Chelerythrine

Chelerythrine (Toddaline, Broussonpapyrine) is a potent, selective antagonist of PKC with an IC50 of 0.66 μM. Chelerythrine also inhibits the BclXL-Bak BH3 peptide binding with an IC50 of 1.5 μM. Chelerythrine shows antitumor, antidiabetic and anti-inflammatory activity.

Nutr Neurosci, 2022, 1-19