Protein Kinase C (PKC)

Cat. No.

A38051

CAS No.

145915-60-2

CGP-53353

Synonyms: DAPH-7

CGP-53353 is a potent protein kinase C (PKC) inhibitor that exhibits IC50 values of 0.41 μM for PKCβII and 3.8 μM for PKCβI. This compound effectively inhibits glucose-induced cell proliferation and DNA synthesis in aortic smooth muscle cells (AoSMC) and A10 cells. CGP-53353 serves as a valuable tool for investigating the mechanisms underlying atherosclerosis in diabetic populations.

Cat. No.

A44089

CAS No.

176504-36-2

Bisindolylmaleimide I hydrochloride

Synonyms: GF109203X hydrochloride; Go 6850 hydrochloride

Bisindolylmaleimide I hydrochloride is a potent and selective inhibitor of Protein Kinase C (PKC), exhibiting inhibition with IC50 values of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ respectively. Additionally, it serves as an inhibitor of Glycogen Synthase Kinase 3 (GSK-3). This compound is valuable in research investigating signal transduction pathways and cell proliferation, making it a crucial tool for studies in cancer, neurobiology, and cardiology.

Cat. No.

A46137

CAS No.

382605-72-3

NSC668394

NSC668394 is a selective inhibitor of ezrin phosphorylation at threonine 567, exhibiting a Kd of 12.59 μM. This compound effectively prevents the phosphorylation of ezrin induced by PKCΙ through direct binding, thereby interfering with key signaling pathways. NSC668394 is primarily utilized in research focused on inhibiting tumor metastasis and studying ezrin's role in cancer progression.

Cat. No.

A46138

CAS No.

120166-69-0

R59949

R59949 is a pan diacylglycerol kinase (DGK) inhibitor that exhibits an IC50 of 300 nM. This compound effectively inhibits the activity of type I DGK α and γ, while also moderately reducing the activity of type II DGK θ and κ. Additionally, R59949 promotes the activation of protein kinase C (PKC) by increasing endogenous diacylglycerol levels. It serves as a valuable tool for studying DGK and PKC signaling pathways in various biological contexts.

Cat. No.

A46139

CAS No.

942425-34-5

PKN1/2-IN-1

PKN1/2-IN-1 is a selective inhibitor of protein kinase N isoforms 1 and 2 (PKN1 and PKN2), demonstrating IC50 values of 16 nM and 210 nM, respectively, along with Ki values of 8 nM and 108 nM. This compound effectively permeates cell membranes and shows significant binding affinity for PKN2, as indicated by NanoBRET assays (IC50 = 2.1 μM). PKN1/2-IN-1 is valuable for investigating physiological processes, particularly in research focused on tumor cell migration and related signaling pathways.

Cat. No.

A46140

CAS No.

86390-77-4

1-Oleoyl-2-acetyl-sn-glycerol

1-Oleoyl-2-acetyl-sn-glycerol is a cell-permeable diacylglycerol (DAG) analog that activates Protein Kinase C (PKC) as its primary target. It is known to induce specific Ca2+ influx through TRPC channels, enhance superoxide production in human neutrophils, and promote the synthesis of phosphatidylinositol 4-phosphate in intact human platelets. Additionally, 1-Oleoyl-2-acetyl-sn-glycerol has been demonstrated to stimulate the proliferation of ascites tumor cells, making it useful for various biochemical and pharmacological studies.

Cat. No.

A46141

CAS No.

1799574-70-1

CC-90005

CC-90005 is a potent and selective inhibitor of protein kinase C-θ (PKC-θ), exhibiting an IC50 of 8 nM. This compound demonstrates considerable selectivity for PKC-θ over PKC-δ, with an IC50 of 4440 nM. CC-90005 effectively inhibits T cell activation by downregulating IL-2 expression, making it a valuable tool for research in immunology and T cell signaling pathways.

Cat. No.

A46142

CAS No.

2238-90-6

Psychosine

Synonyms: Galactosylsphingosine

Psychosine, or galactosylsphingosine, serves as a substrate for the galactocerebrosidase (GALC) enzyme and is recognized as a potential biomarker for Krabbe disease. This cytotoxic lipid is known to induce apoptosis, leading to cell death in various cell types, particularly oligodendrocytes, which are significant in the context of globoid cell leukodystrophy (GLD). Additionally, psychosine acts as an inhibitor of protein kinase C (PKC), further emphasizing its role in cellular signaling pathways and potential applications in neurological research.

Cat. No.

A46143

CAS No.

863987-12-6

ZIP

ZIP is a selective peptide inhibitor of Protein Kinase M zeta (PKMζ), which plays a crucial role in synaptic plasticity and memory processes. This compound effectively impairs morphine-induced conditioned place preference, making it a valuable tool for studying addiction and the molecular mechanisms underlying memory formation. Research applications include investigating the role of PKMζ in memory reinforcement and the modulation of synaptic strength.

Cat. No.

A46144

CAS No.

103883-03-0

Procyanidin A1

Synonyms: Proanthocyanidin A1

Procyanidin A1 is a potent inhibitor of protein kinase C (PKC) activity, effectively blocking degranulation processes in response to PKC activation and calcium influx in RBL-213 mast cells. This compound exhibits significant antiallergic properties, making it valuable for research applications focused on allergic responses and related signaling pathways. Its ability to modulate cellular activities makes Procyanidin A1 a useful tool in studying allergic mechanisms and developing therapeutic strategies.

Cat. No.

A46145

CAS No.

126768-94-3

Myelin Basic Protein

Synonyms: MHP4-14

Myelin Basic Protein (MHP4-14) serves as a specific substrate for protein kinase C (PKC), demonstrating a Km of 7 μM. This synthetic peptide, derived from residues 4-14 of myelin basic protein, is not phosphorylated by various other kinases, including cyclic AMP-dependent protein kinase and casein kinases I and II. It is highly effective for studying PKC activity in crude tissue extracts, providing a low background and reliable results in biochemical assays.

Cat. No.

A46146

CAS No.

15917-65-4

N-Desmethyltamoxifen hydrochloride

N-Desmethyltamoxifen hydrochloride is a prominent inhibitor of protein kinase C (PKC). As the primary metabolite of tamoxifen, it exhibits ten-fold greater potency against PKC compared to its predecessor. Additionally, this compound effectively regulates ceramide metabolism in human acute myeloid leukemia (AML) cells by limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation. Its properties make it valuable for research in cancer biology and metabolic regulation.

Cat. No.

A46147

CAS No.

65914-84-3

1-Stearoyl-2-arachidonoyl-sn-glycerol

1-Stearoyl-2-arachidonoyl-sn-glycerol is a diacylglycerol (DAG) that serves as a potent activator of protein kinase C (PKC). This compound exhibits significant biological activity by enhancing the activity of nonselective cation channels (NSCC). It is commonly utilized in research applications aimed at elucidating PKC-related signaling pathways and assessing the physiological roles of DAG in cellular processes.

Cat. No.

A46148

CAS No.

108930-17-2

Protein kinase inhibitor H-7 dihydrochloride

H-7 dihydrochloride is a potent inhibitor of protein kinase C (PKC), effectively blocking its activity. At a concentration of 100 μM, H-7 dihydrochloride completely inhibits ornithine decarboxylase induction stimulated by both TPA (12-O-tetradecanoylphorbol-13-acetate) and phospholipase C. This reagent is widely utilized in research to investigate PKC-related signaling pathways and its role in cellular processes such as proliferation and differentiation.

Cat. No.

A46149

CAS No.

102649-79-6

SC-10

SC-10 is a potent activator of protein kinase C (PKC), specifically targeting its catalytic activity. This compound enhances PKC signaling pathways, facilitating various cellular processes. SC-10 is widely employed in research applications focusing on cell signaling, cancer biology, and neurobiology, where it helps to elucidate the roles of PKC in cellular growth, differentiation, and apoptosis.

Cat. No.

A46150

CAS No.

35082-49-6

Cercosporin

Synonyms: CGP049090

Cercosporin is a potent protein kinase C (PKC) inhibitor derived from the plant pathogen Pseudocercosporella capsellae. This compound acts as an effective photosensitizer due to its short activation wavelength, making it particularly suitable for superficial photodynamic therapy (PDT) applications where avoiding tissue perforation is crucial. With an IC50 ranging from 0.6 to 1.3 μM, cercosporin showcases significant biological activity in modulating cellular signaling pathways, contributing to its potential utility in cancer research and therapeutic development.

Cat. No.

A46151

CAS No.

12244-57-4

Aurothiomalate sodium

Aurothiomalate sodium is a selective inhibitor of the oncogenic protein kinase C iota (PKCι), demonstrating significant potential in cancer research. This compound effectively inhibits tumor cell proliferation while having minimal effects on cell apoptosis, highlighting its unique mechanism of action. Additionally, Aurothiomalate sodium acts as a potent inhibitor of thioredoxin reductase (TrxR) and possesses anti-tumor properties, making it a valuable tool for investigating signaling pathways involved in cancer biology and therapeutic responses. Its anti-rheumatic properties further extend its relevance in related biomedical studies.

Cat. No.

A46152

CAS No.

2083630-26-4

PS432

PS432 is a selective protein kinase C (PKC) inhibitor, demonstrating IC50 values of 16.9 μM for PKCι and 18.5 μM for PKCζ. This compound effectively reduces the proliferation of non-small cell lung cancer (NSCLC) cells and inhibits tumor growth in mouse xenograft models. It serves as a valuable tool for research applications targeting PKC signaling pathways in cancer biology.

Cat. No.

A46153

CAS No.

84477-87-2

Protein kinase inhibitor H-7

Protein kinase inhibitor H-7 is a selective inhibitor of protein kinase C (PKC) and cyclic nucleotide-dependent protein kinase, exhibiting a Ki of 6 μM for PKC. This compound has been widely used in research to investigate the role of PKC in various cellular processes, including signal transduction and cell proliferation. Additionally, H-7 serves as a valuable tool in studies focused on the modulation of kinases and their associated pathways.

Cat. No.

A46154

CAS No.

331257-53-5

Aprinocarsen sodium

Synonyms: ISIS 3521 sodium

Aprinocarsen sodium is a specific antisense oligonucleotide that targets protein kinase C-alpha (PKC-α), functioning as a potent inhibitor. This 20-mer oligonucleotide modulates cellular processes such as differentiation and proliferation. In vivo studies demonstrate its ability to inhibit the growth of human tumor cell lines in nude mice, highlighting its potential utility as a chemotherapeutic agent in the treatment of various human cancers.

Cat. No.

A46155

CAS No.

137592-45-1

Bisindolylmaleimide II

Synonyms: Bis II

Bisindolylmaleimide II is a potent inhibitor of Protein Kinase C (PKC) isoforms, serving as a valuable tool for dissecting PKC-related signaling pathways. Its inhibitory effect on all PKC subtypes makes it useful in studies investigating cellular processes such as proliferation, differentiation, and apoptosis. This compound is widely applied in research aiming to elucidate the role of PKC in various disease models, including cancer and neurodegenerative disorders.

Cat. No.

A46156

CAS No.

864431-36-7

SBI-0087702

SBI-0087702 is a selective inhibitor of ATF2, primarily targeting its phosphorylation at Thr52 by PKCε. This reagent induces the translocation of ATF2 to the mitochondria in melanoma cells, leading to enhanced apoptosis through the disruption of mitochondrial membrane integrity. Additionally, SBI-0087702 demonstrates significant effects on reducing both the growth and motility of melanoma cells, making it a valuable compound for research into cancer biology and therapeutic applications.

Cat. No.

A46157

CAS No.

88253-86-5

Z-Arg-SBzl

Z-Arg-SBzl is a specific substrate for both bovine and activated human protein C. It effectively facilitates the study of protein C activity and its role in coagulation processes. This compound is valuable for research applications focused on thrombosis and hemostasis, enabling the development of assays to investigate the regulatory mechanisms of blood coagulation.

Cat. No.

A46158

CAS No.

121196-80-3

Myelin basic protein, MBP (68-86)

Myelin basic protein, MBP (68-86), is a peptide derived from the 68th to 86th amino acid residues of the myelin basic protein sequence. This peptide functions as an autoantigen, initiating immune responses that can lead to the destruction of myelin. MBP (68-86) is utilized in the experimental autoimmune encephalomyelitis (EAE) animal model, making it a valuable tool for investigating the immunological mechanisms involved in multiple sclerosis (MS).

Cat. No.

A46159

CAS No.

382148-47-2

Bacopaside I

Bacopaside I is a selective AQP1 inhibitor and protein kinase C (PKC) modulator with notable neuroprotective and anticancer properties. It specifically inhibits the water channel and cGMP-gated ion channel activities of AQP1, thereby reducing the migration of AQP1-expressing colon cancer cells. Additionally, Bacopaside I activates the Akt pathway through PI3K interaction, inhibits MAO-A, and mitigates neuron necrosis and apoptosis due to oxygen-glucose deprivation, while lowering oxidative stress and modulating neuroreceptor expression. This compound is relevant for research in colon cancer, breast cancer, vascular dementia, cerebral ischemia, and associated diseases.