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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.
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.
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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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.
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.
![[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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AJH-836 is an activator of Munc13-1 and protein kinase C (PKC) ε/α, exhibiting a Kd of 4.5 nM for PKCα. This compound facilitates the translocation of Munc13-1 from the cytoplasm to the plasma membrane, thereby enhancing synaptic function. AJH-836 is valuable for research related to neurodegenerative diseases, providing insights into synaptic transmission and neuronal communication.
Synonyms: 1,2-Dioleoyl-rac-glycerol
(±)-1,2-Diolein is a potent activator of protein kinase C (PKC), a crucial regulator of various cellular processes. This compound enhances calcium influx in myotubes, facilitating studies on muscle physiology and signaling pathways. Its application in research supports investigations into PKC-related mechanisms and their implications in muscle function and disease.
1,2-Didecanoylglycerol is a synthetic diacylglycerol that functions as a potent activator of protein kinase C (PKC). It is metabolized by platelets to form 1,2-didecanoylphosphatidic acid (PA10), which plays a crucial role in cellular signaling pathways. This reagent is widely used in research applications involving cell proliferation, differentiation, and various signaling cascades associated with PKC activation.
Gnidimacrin is a protein kinase C (PKC) activator that demonstrates notable anti-proliferative effects on various cancer cell lines. It effectively inhibits growth in human leukemias, stomach cancers, and non-small cell lung cancers in vitro, while also exhibiting antitumor activity against murine leukemias and solid tumors in vivo. This compound can be utilized in research focused on leukemia and solid tumor biology, contributing to the understanding of PKC signaling pathways in cancer therapy.
pTH-Related Protein (1-40) is an activator of the parathyroid hormone receptor (PTHR) and protein kinase C isoforms α and β. This peptide enhances calcium uptake in rat intestinal cells by stimulating the PTHR1 receptor, leading to the upregulation of critical calcium transport proteins, including TRPV6, CaBP-D9k, NCX1, and PMCA1. Its biological activity makes it a valuable tool for research focused on calcium signaling and endocrine regulation in both human and animal models.
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Synonyms: PKC fragment (530-558)
Protein Kinase C (530-558) is a potent activator of Protein Kinase C (PKC). This peptide fragment has been shown to significantly inhibit osteoclastic bone resorption, making it valuable for research on bone metabolism and related disorders. Its specific activation of PKC can provide insights into the signaling pathways involved in various cellular processes, contributing to studies in cell biology and pharmacology.
