PKC Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
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.	Biochem Pharmacol, 2024, 230(Pt 2):116607 Cell Rep, 2023, 42(3):112273 Nat Cardiovasc Res, 2023, 2(6):550-571
S7663	Ruboxistaurin (LY333531) Hydrochloride	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.	Cell Rep Med, 2025, S2666-3791(24)00694-3 JCI Insight, 2025, 10(5)e187315 Nat Commun, 2024, 15(1):8918
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. This compound 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.	Phytomedicine, 2025, 146:157154 Geroscience, 2025, 10.1007/s11357-025-01650-5 Cell Death Discov, 2024, 10(1):263
S6577	PKC-theta inhibitor	PKC-theta inhibitor (compound 20) inhibits PKC-θ with an IC50 of 18 nM.	EMBO J, 2025, 10.1038/s44318-025-00374-8 iScience, 2025, 28(6):112753 JCI Insight, 2023, 8(4)e164793
S1292	Chelerythrine Chloride (NSC 646662)	Chelerythrine Chloride (NSC 646662, Broussonpapyrine) is a potent, selective antagonist of PKC with IC50 of 0.66 μM.	J Headache Pain, 2023, 24(1):49 Nutr Neurosci, 2022, 1-19 J Biol Chem, 2015, 290(34):20841-55
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.	Front Pharmacol, 2024, 15:1372094 Molecules, 2023, 28(3)1444 Molecules, 2021, 26(5)1210
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. This compound also inhibits the BclXL-Bak BH3 peptide binding with an IC50 of 1.5 μM. It shows antitumor, antidiabetic and anti-inflammatory activity.	Nutr Neurosci, 2022, 1-19
S3289	Daphnoretin	Daphnoretin (Dephnoretin, Thymelol), a biologically active compound isolated from Wikstroemia indica C.A. Mey., is a protein kinase C (PKC) activator. This compound 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. This compound is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 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.
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. This compound 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.
E0067	Hispidin	Hispidin is a phenolic compound from Phellinus linteus (a medicinal mushroom) and a potent inhibitor of protein kinase Cβ(PKC) with an IC50 of 2 μM, respectively. It also inhibits beta-secretase (BACE1) and prolyl endopeptidase(PE) with IC50 values of 4.9 μM and 16 μM respectively. It exhibits strong anti-oxidant, anti-cancer, anti-diabetic, anti-dementia, anti-inflammatory, anti-apoptotic, and antiviral properties.
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. This compound inhibits intimal thickening after balloon injury to rat carotid arteries, and inhibits PKC activation induced by PDGF.
E2510	WAY-301398	WAY-301398 (6-methoxynaphthalene) can bind to protein kinase C (PKC).
E6517^New	PKN1	PKN1/2-IN-1 is a cell-permeable compound that inhibits PKN1 and PKN2, with IC50 values of 16 nM and 210 nM, and Ki values of 8 nM and 108 nM, respectively. In NanoBRET assays, it shows intracellular PKN2 binding with an IC50 of 2.1 μM. This compound is applicable for investigating tumor cell migration and related physiological processes.
S7859	WAY-354831	WAY-354831 exhibits antibacterial activity.
E5794	Ionomycin calcium	Ionomycin calcium (SQ23377 calcium) is a potent and selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. It is highly specific for divalent cations (Ca>Mg>Sr=Ba) and also promotes T cell activation and proliferation by inducing phosphoinositide hydrolysis and protein kinase C (PKC) activation, leading to IL-2 production and IL-2R expression.
E3408	Radix Euphorbiae Ebracteolatae Extract	Radix Euphorbiae Ebracteolatae Extract is extracted from Radix Euphorbiae Ebracteolatae, which modulates aquaporins via inhibiting PKC activity in the kidney.
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. It also exerts 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.
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.	Theranostics, 2025, 15(18):9819-9837 Cell Rep, 2025, 44(7):115947 Front Cell Infect Microbiol, 2025, 15:1543186
S1573	Fasudil (HA-1077) Hydrochloride	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.	Stem Cell Res Ther, 2025, 16(1):597 Transl Oncol, 2025, 51:102209 J Immunother Cancer, 2024, 12(11)e009805
S2485	Mitoxantrone Dihydrochloride (NSC 301739)	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.	Aging Cell, 2025, e70075 Biol Open, 2025, 14(9)bio062175 J Immunother Cancer, 2024, 12(11)e009805
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.	Proc Natl Acad Sci U S A, 2025, 122(8):e2421717122 Cell Mol Life Sci, 2025, 82(1):201 Commun Biol, 2025, 8(1):607
S7074	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.	Protein Cell, 2025, pwaf020 Nat Commun, 2025, 16(1):8054 Cancer Commun (Lond), 2025, 10.1002/cac2.70036
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
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. This compound 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. This compound also inhibits PKA with IC50 of 11.8μM. It is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with IC50 of 0.2 μM.	Elife, 2021, 10e68473
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.	Cell Rep Med, 2025, 6(8):102297
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
E7852	CKI-7	CKI-7 (CKI-7 2HCl) is an inhibitor of casein kinase 1 (CK1) with ki of 8.5 μM and IC50 of 6 μM. It is selective for CK1 over CK2, PKC, CaM kinase II (CaMKII), and cyclic AMP-dependent protein kinase (PKA) with IC50 of 90, >1000, 195, and 550 μM, respectively. This compound also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1).
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. This compound drives abnormal aggregation of protein kinase C iota (PKCι) in nucleus of sensitive cells but not in resistant cells.
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.