PKC

シグナル伝達経路

PKCシグナル伝達経路

PKC製品

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  • PKC阻害剤 (35)
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S1421 Staurosporine (STS) スタウロスポリン (Staurosporine (AM-2282、Antiviotic AM-2282、STS)) は、PKCα、PKCγ、および PKCη に対する強力な PKC 阻害剤であり、IC50 は 2 nM、5 nM、および 4 nM です。 無細胞アッセイでは、PKCδ (20 nM)、PKCε (73 nM) に対して効力が低く、PKCζ (1086 nM) に対してほとんど活性がありません。 また、PKA、PKG、S6K、CaMKII などの他のキナーゼに対しても阻害活性を示します。臨床フェーズ3。
Nat Commun, 2024, 15(1):489
Nat Commun, 2024, 15(1):1300
Mol Syst Biol, 2024, 20(1):28-55
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.
Cancer Res, 2023, 83(19):3237-3251
Biomed Pharmacother, 2023, 158:114176
Cancer Metab, 2023, 11(1):26
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.
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101244
Cell Rep, 2023, 42(3):112273
Elife, 2023, 12e83345
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.
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101244
Cell Rep, 2023, 42(3):112273
Cell Rep, 2023, 42(3):112273
S1573 Fasudil HCl Fasudil HCl, 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.
PeerJ, 2023, 11:e15494
Alcohol, 2023, 115:5-12
medRxiv, 2023, 10.1101/2023.12.19.23299785
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.
Nat Cell Biol, 2022, 24(1):88-98
Oncogene, 2022, 10.1038/s41388-022-02179-z
Cancers (Basel), 2022, 14(21)5215
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.
Nat Commun, 2023, 14(1):4062
J Clin Invest, 2023, 10.1172/JCI163591
Nat Commun, 2023, 14(1):4062
S7791 PMA (Phorbol 12-myristate 13-acetate) PMA (Phorbol 12-myristate 13-acetate), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P).
Cancer Commun (Lond), 2023, 43(8):909-937
Cell Rep, 2023, 42(8):112944
Elife, 2023, 12e85494
S2485 Mitoxantrone 2HCl Mitoxantrone 2HCl 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.
Mol Metab, 2024, 80:101873
Cell Commun Signal, 2023, 21(1):167
Int J Mol Sci, 2023, 10.3390/ijms242216375
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.
Blood, 2023, 141(9):1023-1035
Nat Commun, 2023, 14(1):5709
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
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. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
MedComm (2020), 2023, 4(5):e346
MedComm -2020), 2023, 4(5):e346
Aging Cell, 2023, e13771.
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.
J Cell Sci, 2023, 136(4)jcs259788
Sci Adv, 2023, 9(34):eadi5168
Sci Adv, 2023, 9(34):eadi5168
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.
Cell Rep, 2023, 42(3):112273
Elife, 2022, 11e80953
Cell Oncol (Dordr), 2022, 10.1007/s13402-022-00673-w
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.
Life Sci, 2023, 329:121972
bioRxiv, 2023, 10.1101/2023.12.07.570359
Cell Rep Methods, 2023, 3(10):100599
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.
Ecotoxicol Environ Saf, 2023, 257:114940
Mol Biol Cell, 2023, 34(8):ar79
Nat Commun, 2022, 13(1):1768
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.
Mol Metab, 2023, 70:101694
ACS Appl Mater Interfaces, 2022, 14(21):24144-24159
Biomed Pharmacother, 2022, 145:112437
S6577 PKC-theta inhibitor PKC-theta inhibitor (compound 20) inhibits PKC-θ with an IC50 of 18 nM.
JCI Insight, 2023, 8(4)e164793
Int J Mol Sci, 2023, 24(15)11970
Commun Biol, 2022, 5(1):795
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
S1292 Chelerythrine Chloride (NSC 646662) Chelerythrine Chloride (NSC 646662, Broussonpapyrine) is a potent, selective antagonist of PKC with IC50 of 0.66 mM.
J Headache Pain, 2023, 24(1):49
Nutr Neurosci, 2022, 1-19
J Biol Chem, 2015, 290(34):20841-55
S6723 Darovasertib (LXS-196) Darovasertib (LXS-196, IDE-196) is a selective inhibitor of protein kinase C (PKC).
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101244
Cell Mol Biol Lett, 2023, 28(1):24
Commun Biol, 2022, 5(1):795
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.
Nat Commun, 2024, 15(1):686
Neoplasia, 2020, 22(10):470-483
Vet Microbiol, 2020, 251:108913
S2327 Myricitrin Myricitrin (Myricitrine), a flavonoid compound isolated from the root bark of Myrica cerifera, which exerts antinociceptive effects.
Molecules, 2023, 28(3)1444
Molecules, 2021, 26(5)1210
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
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 11.8 μM.
Elife, 2021, 10e68473
S9101 Ingenol Ingenol, a plant-derived diterpenoid, is a weak PKC activator and possesses important anticancer activity.
Sci Rep, 2020, 10(1):13124
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
E0124 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
S7074New Ionomycin Ionomycin (SQ23377) is a potent and selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. It induces the activation of protein kinase C (PKC) and promotes apoptosis.
Am J Physiol Cell Physiol, 2020, 10.1152/ajpcell.00290.2020
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.
S9522 Valrubicin Valrubicin(AD-32) is a chemotherapy drug used to treat bladder cancer. Valrubicin inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 μM and 1.25 μM, respectively.
S3819 Decursinol angelate Decursinol angelate is a cytotoxic and protein kinase C activating agent from the root of Angelica gigas.
E2368 N-Desmethyltamoxifen hydrochloride N-Desmethyltamoxifen hydrochloride (N-Desmethyl tamoxifen HCl), the primary metabolite of tamoxifen, is an estrogen response modifer and protein kinase C inhibitor with IC50 of 25 µM.
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.
E0010 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.
E2403 ζ-Stat (NSC37044) ζ-Stat (NSC37044) is a specific and atypical protein kinase Cζ (PKCζ) inhibitor, with an IC50 of 5 μM.
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.
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.
S2323 Methyl-Hesperidin Methyl Hesperidin is a flavanone glycoside (flavonoid) (C28H34O15) found abundantly in citrus fruits. Its aglycone form is called hesperetin.
E2506 A-3 hydrochloride A-3 hydrochloride, a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases, againsts cAMP-dependent protein kinase (PKA) (Ki=4.3 µM), casein kinase II (CK2) (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM), also inhibits Protein Kinase C (PKC) and casein kinase I (CK1) with Ki values of 47 µM and 80 µM, respectively.
S6214 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.
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.
Adv Sci (Weinh), 2024, 11(4):e2304987
E2839 Bisindolylmaleimide VIII (acetate) Bisindolylmaleimide VIII (acetate) (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC, also exerting IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively.
E0786 N-Desmethyltamoxifen N-Desmethyltamoxifen, the major metabolite of Tamoxifen in humans and a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen, also is a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
S1421 Staurosporine (STS) スタウロスポリン (Staurosporine (AM-2282、Antiviotic AM-2282、STS)) は、PKCα、PKCγ、および PKCη に対する強力な PKC 阻害剤であり、IC50 は 2 nM、5 nM、および 4 nM です。 無細胞アッセイでは、PKCδ (20 nM)、PKCε (73 nM) に対して効力が低く、PKCζ (1086 nM) に対してほとんど活性がありません。 また、PKA、PKG、S6K、CaMKII などの他のキナーゼに対しても阻害活性を示します。臨床フェーズ3。
Nat Commun, 2024, 15(1):489
Nat Commun, 2024, 15(1):1300
Mol Syst Biol, 2024, 20(1):28-55
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.
Cancer Res, 2023, 83(19):3237-3251
Biomed Pharmacother, 2023, 158:114176
Cancer Metab, 2023, 11(1):26
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.
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101244
Cell Rep, 2023, 42(3):112273
Elife, 2023, 12e83345
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.
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101244
Cell Rep, 2023, 42(3):112273
Cell Rep, 2023, 42(3):112273
S1573 Fasudil HCl Fasudil HCl, 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.
PeerJ, 2023, 11:e15494
Alcohol, 2023, 115:5-12
medRxiv, 2023, 10.1101/2023.12.19.23299785
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.
Nat Cell Biol, 2022, 24(1):88-98
Oncogene, 2022, 10.1038/s41388-022-02179-z
Cancers (Basel), 2022, 14(21)5215
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.
Nat Commun, 2023, 14(1):4062
J Clin Invest, 2023, 10.1172/JCI163591
Nat Commun, 2023, 14(1):4062
S2485 Mitoxantrone 2HCl Mitoxantrone 2HCl 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.
Mol Metab, 2024, 80:101873
Cell Commun Signal, 2023, 21(1):167
Int J Mol Sci, 2023, 10.3390/ijms242216375
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.
Blood, 2023, 141(9):1023-1035
Nat Commun, 2023, 14(1):5709
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
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. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
MedComm (2020), 2023, 4(5):e346
MedComm -2020), 2023, 4(5):e346
Aging Cell, 2023, e13771.
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.
J Cell Sci, 2023, 136(4)jcs259788
Sci Adv, 2023, 9(34):eadi5168
Sci Adv, 2023, 9(34):eadi5168
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.
Cell Rep, 2023, 42(3):112273
Elife, 2022, 11e80953
Cell Oncol (Dordr), 2022, 10.1007/s13402-022-00673-w
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.
Life Sci, 2023, 329:121972
bioRxiv, 2023, 10.1101/2023.12.07.570359
Cell Rep Methods, 2023, 3(10):100599
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.
Ecotoxicol Environ Saf, 2023, 257:114940
Mol Biol Cell, 2023, 34(8):ar79
Nat Commun, 2022, 13(1):1768
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.
Mol Metab, 2023, 70:101694
ACS Appl Mater Interfaces, 2022, 14(21):24144-24159
Biomed Pharmacother, 2022, 145:112437
S6577 PKC-theta inhibitor PKC-theta inhibitor (compound 20) inhibits PKC-θ with an IC50 of 18 nM.
JCI Insight, 2023, 8(4)e164793
Int J Mol Sci, 2023, 24(15)11970
Commun Biol, 2022, 5(1):795
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
S1292 Chelerythrine Chloride (NSC 646662) Chelerythrine Chloride (NSC 646662, Broussonpapyrine) is a potent, selective antagonist of PKC with IC50 of 0.66 mM.
J Headache Pain, 2023, 24(1):49
Nutr Neurosci, 2022, 1-19
J Biol Chem, 2015, 290(34):20841-55
S6723 Darovasertib (LXS-196) Darovasertib (LXS-196, IDE-196) is a selective inhibitor of protein kinase C (PKC).
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101244
Cell Mol Biol Lett, 2023, 28(1):24
Commun Biol, 2022, 5(1):795
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.
Nat Commun, 2024, 15(1):686
Neoplasia, 2020, 22(10):470-483
Vet Microbiol, 2020, 251:108913
S2327 Myricitrin Myricitrin (Myricitrine), a flavonoid compound isolated from the root bark of Myrica cerifera, which exerts antinociceptive effects.
Molecules, 2023, 28(3)1444
Molecules, 2021, 26(5)1210
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
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 11.8 μM.
Elife, 2021, 10e68473
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
S9522 Valrubicin Valrubicin(AD-32) is a chemotherapy drug used to treat bladder cancer. Valrubicin inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 μM and 1.25 μM, respectively.
E2368 N-Desmethyltamoxifen hydrochloride N-Desmethyltamoxifen hydrochloride (N-Desmethyl tamoxifen HCl), the primary metabolite of tamoxifen, is an estrogen response modifer and protein kinase C inhibitor with IC50 of 25 µM.
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.
E0010 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.
E2403 ζ-Stat (NSC37044) ζ-Stat (NSC37044) is a specific and atypical protein kinase Cζ (PKCζ) inhibitor, with an IC50 of 5 μM.
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.
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.
S6214 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.
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.
Adv Sci (Weinh), 2024, 11(4):e2304987
E2839 Bisindolylmaleimide VIII (acetate) Bisindolylmaleimide VIII (acetate) (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC, also exerting IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively.
E0786 N-Desmethyltamoxifen N-Desmethyltamoxifen, the major metabolite of Tamoxifen in humans and a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen, also is a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
S7791 PMA (Phorbol 12-myristate 13-acetate) PMA (Phorbol 12-myristate 13-acetate), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P).
Cancer Commun (Lond), 2023, 43(8):909-937
Cell Rep, 2023, 42(8):112944
Elife, 2023, 12e85494
S9101 Ingenol Ingenol, a plant-derived diterpenoid, is a weak PKC activator and possesses important anticancer activity.
Sci Rep, 2020, 10(1):13124
S7074New Ionomycin Ionomycin (SQ23377) is a potent and selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. It induces the activation of protein kinase C (PKC) and promotes apoptosis.
Am J Physiol Cell Physiol, 2020, 10.1152/ajpcell.00290.2020
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.
E0124 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
E2506 A-3 hydrochloride A-3 hydrochloride, a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases, againsts cAMP-dependent protein kinase (PKA) (Ki=4.3 µM), casein kinase II (CK2) (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM), also inhibits Protein Kinase C (PKC) and casein kinase I (CK1) with Ki values of 47 µM and 80 µM, respectively.
S7074New Ionomycin Ionomycin (SQ23377) is a potent and selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. It induces the activation of protein kinase C (PKC) and promotes apoptosis.
Am J Physiol Cell Physiol, 2020, 10.1152/ajpcell.00290.2020

PKC阻害剤の選択性比較

Tags: PKC inhibitor|PKC agonist|PKC activator|PKC inducer|PKC antagonist|PKC signaling pathway|PKC assay kit