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Protein kinase C (PKC) inhibitors and activators act on a family of lipid-regulated serine/threonine kinases. Conventional PKC isoforms require calcium and diacylglycerol, novel isoforms need only diacylglycerol, and atypical isoforms respond to neither. Tumor-promoting phorbol esters mimic diacylglycerol and were shown in 1982 to activate PKC directly. 12-O-tetradecanoyl phorbol-13-acetate (TPA) is the standard activator of this kind, and ingenol mebutate also activates several isoforms. Staurosporine was first described as a PKC inhibitor but blocks a wide range of protein kinases. Enzastaurin is selective for PKCβ, while GO6983 and Ro 31-8220 mesylate inhibit multiple conventional and novel isoforms.
Synonyms: PEP005; ingenol-3-angelate; I3A
Ingenol mebutate is a substance found in the sap of the plant Euphorbia peplus and an inducer of cell death.
Synonyms: Indolactam V
(-)-Indolactam V is a protein kinase C activator, which strongly directs human ES cell-derived definitive endoderm into pancreatic endoderm.
Synonyms: PKC Activator V
alpha-Amyloid Precursor Protein Modulator is a cell-permeable benzolactam derived PKC activator (Ki = 11.9 nM for PKCα) that efficiently enhances non-amyloidogenic α-processing of amyloid precursor protein (APP) even at 100 nM in human fibroblas.
Synonyms: TPA; Phorbol 12-myristate 13-acetate
12-O-tetradecanoyl phorbol-13-acetate is a diester of phorbol and is a tumor promoting compound extracted from croton oil. It is a reversible, highly potent protein kinase C (PKC) activator in vitro and in vivo at nM concentrations.
Synonyms: Erythrosphingosine; erythro-C18-Sphingosine; trans-4-Sphingenine
D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
Roy-Bz is a selecive PKCδ activator. Roy-Bz potently inhibits the proliferation of colon cancer cells by inducing a PKCδ-dependent mitochondrial apoptotic pathway involving caspase-3 activation.
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Synonyms: NSC 623310; Stillingia Factor S7
Prostratin is a protein kinase C activator found in the bark of the mamala tree of Samoa, Homalanthus nutans.
![[Ser25] Protein Kinase C (19-31)](https://www.adooq.com/media/catalog/product/cache/16359f9c8ddfa823fcb5503b1e11b7ae/a/1/a14882-protein-kinase-c-_19-31_.gif)
Protein Kinase C (19-31), this peptide derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, it was used as protein kinase C substrate peptide for testing the protein kinase C activity.
Synonyms: (-)-Ingenol
Ingenol is a potent activator of protein kinase C (PKC), exhibiting a Ki value of 30 μM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Ingenol can be utilized to explore the role of PKC in various signaling pathways and to investigate its potential therapeutic applications in oncology.
Synonyms: Phorbol dibutyrate; PDBu
Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator and a potent skin tumor promoter.
Synonyms: DCPLA methyl ester
DCPLA-ME, the methyl ester form of DCPLA, is a potent PKCε activator for use in the treatment of neurodegenerative diseases.
Decursinol angelate, a cytotoxic and protein kinase C (PKC) activating agent from the root of Angelica gigas, possesses anti-tumor and anti-inflammatory activities.
Synonyms: PKC (19-31)
Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.
OSU-2S is a potent activator of Protein Kinase C delta (PKCδ). It effectively inhibits cell proliferation and migration while inducing apoptosis. In combination with Sorafenib, OSU-2S decreases the phosphorylation of ERK1/2 and enhances PKCδ expression (38 kDa). Additionally, OSU-2S is a non-immunosuppressive analogue of FTY720 and demonstrates notable anticancer activity, making it valuable for cancer research applications.
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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.
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.
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.
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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.
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.
1,2-Didecanoyl-sn-glycerol is a potent activator of protein kinase C (PKC), serving as an analog of the second messenger diacylglycerol (DAG). This compound is anticipated to elicit biological activities akin to those of 1,2-dioctanoyl-sn-glycerol, making it valuable for investigating PKC signaling pathways. Researchers can utilize 1,2-didecanoyl-sn-glycerol in studies focused on cellular processes influenced by PKC activation, contributing to the understanding of various physiological and pathological conditions.
Synonyms: NCM 119
SC-9 is a potent activator of protein kinase C (PKC) in the presence of calcium ions (Ca2+). This compound is instrumental in studying the Ca2+-dependent signaling pathways regulated by PKC. Its ability to modulate these pathways makes SC-9 valuable for research applications related to cell proliferation, differentiation, and various disease models.
Synonyms: Ingenol 3-benzoate
Ingenol 3-monobenzoate is an aversion inducer that selectively activates protein kinase C (PKC) with a Ki of 0.14 nM. This compound inhibits the expression of phosphoenolpyruvate carboxykinase, leading to reduced gluconeogenesis and elevated cortisol levels, which collectively contribute to induced food aversion. Ingenol 3-monobenzoate is valuable for research into behavioral responses to aversive stimuli and the underlying metabolic mechanisms.
Bryostatin 3 is a macrocyclic lactone that serves as a potent protein kinase C (PKC) activator, exhibiting a Ki value of 2.75 nM. This compound has been shown to inhibit the effects of 12-O-tetradecanoylphorbol-13-acetate (TPA) on cell proliferation while maintaining TPA-stimulated cell-substratum adhesion. Bryostatin 3 is widely utilized in research applications focusing on the modulation of PKC activity and its implications in cancer biology and cell signaling pathways.
EGFR Peptide is a selective substrate for Protein Kinase C (PKC), facilitating the measurement of PKC activity in various biological contexts. This peptide is instrumental in studies examining PKC's role in cellular signaling pathways, making it a valuable tool for researchers exploring cancer biology, cell proliferation, and differentiation processes. Its specific interaction with PKC allows for accurate assessments of enzyme activity, contributing to a deeper understanding of PKC-mediated signaling mechanisms.
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All 3 sizes![[Glu27]-PKC (19-36)](https://www.adooq.com/media/catalog/product/cache/16359f9c8ddfa823fcb5503b1e11b7ae/a/4/a46188-glu27-pkc-19-36.gif)
[Glu27]-PKC (19-36) is a peptide that serves as an inactive control for protein kinase C (PKC) (19-36). As a pseudosubstrate peptide inhibitor, it is designed to maintain PKC in an inactive state without the presence of allosteric activators, such as phospholipids. This reagent is applicable in studies examining the regulation of PKC activity and its role in various cellular signaling pathways. Researchers can utilize [Glu27]-PKC (19-36) to assess the impact of active and inactive states of PKC in experimental setups.
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