Catalog No.
Product Name
Application
Product Information
Citations
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PKC Inhibitor
Sphingosine (d14:1), also known as Tetradecasphing-4-enine, is a selective inhibitor of Protein Kinase C (PKC). This sphingolipid disrupts the interaction between PKC and sn-1,2-diacylglycerol (DAG) or phorbol esters, thereby modulating signaling pathways. Sphingosine (d14:1) is primarily utilized in research investigating cellular processes regulated by PKC, including cell proliferation, differentiation, and apoptosis. -
PKC Activator
Sapintoxin D is a fluorescent phorbol ester that activates protein kinase C (PKC) in a calcium-dependent manner. This compound is instrumental for studying PKC's role in various cellular processes and signal transduction pathways. Its fluorescent properties facilitate real-time monitoring of PKC activity, making it valuable for research applications in cancer biology and neurobiology. -
PKC Activator
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. -
Midostaurin's Active Metabolite
O-Desmethyl Midostaurin is the active metabolite of Midostaurin, produced through cytochrome P450 liver enzyme metabolism. This compound serves as a valuable biomarker for assessing Midostaurin metabolism in vivo. Additionally, Midostaurin itself is known for being a multi-targeted protein kinase inhibitor, demonstrating IC50 values ranging from 22-500 nM. O-Desmethyl Midostaurin can be utilized in various biological studies concerning drug metabolism and pharmacokinetics. -
PKC Inhibitor
Bisindolylmaleimide XI hydrochloride is a potent and selective inhibitor of protein kinase C (PKC) with IC50 values of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCε, respectively. This compound is orally active, making it a valuable tool for exploring the role of PKC in various cell signaling pathways. Its application spans cancer research, neurobiology, and cardiovascular studies, providing insights into PKC-mediated processes and potential therapeutic targets. -
Stable Isotope
Psychosine-d5 is a deuterium-labeled analog of Psychosine, a substrate for the galactocerebrosidase (GALC) enzyme. This stable isotope serves as a potential biomarker for Krabbe disease and is utilized in research to study the disease's pathophysiology. As a highly cytotoxic lipid, Psychosine can induce cell death across various cell types, making Psychosine-d5 valuable for investigations into cell toxicity and lipid metabolism. -
iNOS/ PKC-θ Dual Inhibitor
(Rac)-Anemonin is a dual inhibitor targeting inducible nitric oxide synthase (iNOS) and protein kinase C theta (PKC-θ). It selectively inhibits iNOS while also reducing the stability of the PKC-θ protein, showcasing significant biological activity. Research indicates that (Rac)-Anemonin can alleviate symptoms in dextran sodium sulfate-induced acute ulcerative colitis in murine models, making it valuable for studying inflammation-related diseases. -
PKCβ Inhibitor
Ruboxistaurin mesylate is a selective and ATP-competitive inhibitor of protein kinase C-beta (PKCβ) with IC50 values of 4.7 nM and 5.9 nM for the PKCβI and PKCβII isoforms, respectively. This compound shows potential in the study of several pathological conditions, including eye disorders, heart failure, and diabetes. Its specific inhibition of PKCβ can facilitate investigations into the underlying mechanisms of these diseases and the development of targeted therapeutic strategies. -
PKC Inhibitor
N-Desmethyltamoxifen, a potent protein kinase C (PKC) inhibitor, is the primary metabolite of tamoxifen in humans. It demonstrates significantly enhanced PKC inhibitory activity, being ten-fold more potent than its precursor. Additionally, N-Desmethyltamoxifen effectively regulates ceramide metabolism in human acute myeloid leukemia (AML) cells, influencing ceramide glycosylation, hydrolysis, and sphingosine phosphorylation, making it a valuable tool for cancer research and therapeutic studies. -
Mitofusin 1-βIIPKC Inhibitor
SAMβA is a selective inhibitor targeting the interaction between mitofusin 1 and βIIPKC. This compound is conjugated to the cell-permeable peptide TAT47-57, facilitating its penetration into cells. SAMβA has demonstrated potential in enhancing heart failure outcomes in rat models, making it a valuable tool for investigating mitochondrial dynamics and associated pathophysiological processes in cardiac research. -
TPA Negative Control
4α-TPA is an inactive analog of TPA, serving as a negative control in TPA-mediated experiments. This reagent is critical for distinguishing specific TPA-activated events from non-specific responses in biological assays. It aids researchers in validating experimental outcomes related to TPA signaling pathways and discerning the effects of TPA on various cellular processes. -
PKC Inhibitor
NPC-15437 dihydrochloride is a selective and reversible inhibitor of protein kinase C (PKC), demonstrating an IC50 value of 19 μM. This compound has been shown to impact the mechanisms associated with memory consolidation, making it a valuable tool for studying cognitive processes and neurobiology. Its penetrative properties enable effective investigation in various biological systems. -
Bioactive Peptide
PKCε (85-92) is a bioactive peptide that selectively activates epsilon protein kinase C (e-PKC). This peptide effectively induces MARCKS phosphorylation in wild-type cells, demonstrating its role in signaling pathways related to cellular function. However, it does not influence MARCKS phosphorylation in cells derived from knockout mice, indicating its specificity. PKCε (85-92) is valuable for research applications focused on PKC signaling and the study of related cellular processes. -
Balanced Vasodilator
Flosequinan is a balanced vasodilator that effectively reduces systemic vascular resistance while simultaneously decreasing the left ventricular afterload and arterial wave reflection. Its unique mechanism aids in alleviating the beating component of left ventricular afterload, making it a valuable tool for research in acute heart failure. This compound offers insight into the hemodynamic changes associated with various cardiovascular conditions, facilitating the study of potential therapeutic interventions. -
PKC Inhibitor
(S)-Ro 32-0432 is a selective, orally active inhibitor of protein kinase C (PKC), exhibiting ATP-competitive properties. Its IC50 values demonstrate high potency against various PKC isoforms, including PKCα (9.3 nM) and PKCβI (28 nM). Additionally, (S)-Ro 32-0432 acts as an inhibitor of G protein-coupled receptor kinase 5 (GRK5). This compound is valuable for investigating T-cell activation mechanisms and is relevant for research in chronic inflammatory and autoimmune diseases. -
PKC Activator
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. -
PKC Inhibitor
N-myristoyl-RKRTLRRL is a potent inhibitor of Protein Kinase C (PKC), specifically targeting the binding of PKC substrates. This compound effectively inhibits calcium- and phosphatidylserine-dependent histone phosphorylation, demonstrating an IC50 of 5 µM. It serves as a valuable tool for research into PKC-related signaling pathways and the mechanisms of histone modification in various biological contexts. -
Aversion Inducer
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. -
Stable Isotope
Ruboxistaurin-d6 hydrochloride is a deuterated form of Ruboxistaurin hydrochloride, a selective inhibitor of protein kinase C (PKC) beta. Exhibiting ATP-dependent competitive inhibition, it demonstrates significant potency with a Ki of 2 nM and an IC50 of 4.7 nM for PKC beta I and 5.9 nM for PKC beta II. This stable isotope is valuable for research applications involving metabolic tracing, pharmacokinetics, and the study of PKC-related cellular signaling pathways. -
Stable Isotope
1-Stearoyl-2-Arachidonoyl-d8-sn-Glycerol is a deuterium-labeled derivative of 1-Stearoyl-2-arachidonoyl-sn-glycerol, a diacylglycerol (DAG) that includes polyunsaturated fatty acids. This compound is known to activate protein kinase C (PKC) and enhance the activity of nonselective cation channels (NSCC). It serves as a valuable tool for studying lipid signaling pathways and the regulation of cellular processes in various research applications. -
PKC Activator
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. -
PKC Inhibitor
PKC-IN-4 is a selective inhibitor of atypical protein kinase C (aPKC) with an IC50 of 0.52 µM. This compound effectively inhibits TNF-α-induced NF-κB signaling in vitro, making it a valuable tool for studies involving inflammatory responses. Additionally, PKC-IN-4 has been shown to block VEGF- and TNF-α-induced permeability across the retinal vasculature, highlighting its potential in retinal disease research and vascular permeability exploration. -
PKC-ι Inhibitor
PKCiota-IN-2 is a potent inhibitor of Protein Kinase C iota (PKC-ι), exhibiting an IC50 value of 2.8 nM. In addition to its primary target, PKCiota-IN-2 also demonstrates inhibitory activity against PKC-α and PKC-ε with IC50 values of 71 nM and 350 nM, respectively. This compound is valuable for research applications exploring the role of PKC isoforms in signal transduction, cancer, and other diseases. -
PKC Inhibitor
NA 0345 is a potent protein kinase C (PKC) inhibitor, exhibiting IC50 values of 70 nM in the presence of 12-O-tetradecanoyl-13-acetate and 110 nM in its absence. This compound selectively inhibits PKC activity, effectively reducing the positive inotropic effects associated with α1-adrenergic receptors. NA 0345 is useful in research applications aimed at elucidating the role of PKC in cardiovascular function and signal transduction pathways. -
PKC Substrate
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. -
Peptide
[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. -
Munc13-1/PKC ε/α Activator
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. -
iNOS/ PKC-θ Dual Inhibitor
Anemonin is a dual inhibitor targeting inducible nitric oxide synthase (iNOS) and protein kinase C theta (PKC-θ). This compound significantly reduces the translation and enhances the protein stability of PKC-θ, demonstrating potent anti-inflammatory effects. Anemonin has been shown to alleviate symptoms of dextran sodium sulfate-induced acute ulcerative colitis in murine models, making it a valuable tool for researching inflammation-related diseases. -
PKC activator
(±)-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. -
Peptide
Protein Kinase C β Peptide is a peptide fragment derived from Protein Kinase Cβ, which plays a critical role in regulating vascular function. It has been shown that hyperglycemia negatively impacts endothelium-derived nitric oxide production, leading to impaired vasodilation. The inhibition of Protein Kinase Cβ can counteract the reduction in endothelium-dependent vasodilation that occurs during acute hyperglycemia, making this peptide a valuable tool for research into vascular complications associated with diabetes and metabolic disorders. -
PKC Inhibitor
(S)-Ro 32-0432 free base is a selective and potent ATP-competitive inhibitor of Protein Kinase C (PKC), with IC50 values of 9.3 nM for PKCα, 28 nM for PKCβI, 30 nM for PKCβII, 36.5 nM for PKCγ, and 108.3 nM for PKCε. Additionally, it acts as a selective inhibitor of G protein-coupled receptor kinase 5 (GRK5). (S)-Ro 32-0432 free base effectively inhibits T-cell activation, making it a valuable tool for research into chronic inflammatory and autoimmune diseases. -
PKC Activator
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. -
PKC Activator
ɛPKC(85–92), Myristoylated is a cell-permeable peptide that activates Protein Kinase C (PKC) through myristoylation. This compound enhances nitric oxide (NO) release in cultured human umbilical vein endothelial cells (HUVECs), making it a valuable tool for investigating endothelial cell function and signaling pathways. Research applications include studies on vascular biology and the modulation of PKC activity in various physiological and pathological processes. -
PKC Activator
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. -
PKCη Pseudosubstrate Inhibitor
PKCη pseudosubstrate inhibitor, myristoylated is a cell-permeable compound designed to inhibit protein kinase C eta (PKCη) activity by mimicking its substrate. This inhibitor allows for the exploration of PKCη’s role in various signaling pathways, facilitating studies on its biological functions in cell proliferation, differentiation, and apoptosis. Researchers can utilize this tool to investigate the therapeutic potential of modulating PKCη activity in various diseases. -
Bioactive Peptide
KRPpSQRHGSKY-NH2 is a bioactive peptide that serves as a phosphorylated substrate for protein kinase C (PKC). This compound is utilized in research applications to study signaling pathways and phosphorylation events mediated by PKC. Its role in cellular processes makes it valuable for investigating various biological functions and potential therapeutic targets. -
Anti-cancer Aent
CP-46665 dihydrochloride is an anticancer agent that primarily targets cellular proliferation. It inhibits the incorporation of tritiated thymidine into leukemia cells and various human solid tumor cells in vitro. This compound leads to the loss of surface characteristics in tumor cells and disrupts cell membranes, thereby effectively inhibiting cell growth and proliferation. It is a valuable tool for research applications focused on cancer biology and therapeutic development. -
PKC Inhibitor
PS315 is an allosteric inhibitor of protein kinase C (PKC) that targets the PIF-pocket of atypical PKC isoforms. By inducing a displacement of the active site residue Lys111, PS315 effectively inhibits both full-length PKCζ (IC50 = 10 µM) and PKCη (IC50 = 30 µM). This compound has demonstrated anti-cancer properties, making it a valuable tool for research into PKC-related signaling pathways and cancer therapeutics. -
PKCTheta Inhibitor
PKCTheta-IN-1 is a selective inhibitor of Protein Kinase C Theta (PKCθ), exhibiting an IC50 value of 0.1 nM. This compound disrupts PKCθ-mediated signaling pathways, contributing to its potential in immunological research and cellular proliferation studies. Its specificity makes it a valuable tool for investigating the role of PKCθ in T-cell activation and other related processes. -
PKC βII V5 Peptide
Protein Kinase C (660-673) is a peptide derived from the PKC βII isoform, specifically designed to exhibit RACK1-binding affinity. This peptide serves as a valuable tool for studying the interactions of PKC βII with RACK1, providing insights into signaling pathways mediated by Protein Kinase C. Its unique structural properties make it suitable for investigating PKC βII's role in cellular processes, including proliferation and differentiation. -
PKC Inhibitor
PKC-IN-7 is a selective inhibitor of protein kinase C (PKC). This compound demonstrates significant anti-proliferative effects in various cancer cell lines and is valuable for investigating the role of PKC in cancer signaling pathways. It is suitable for research applications focused on tumor biology, cell signaling, and therapeutic development for PKC-related diseases. -
PKC Inhibitor
6-Deoxyisojacareubin is a specific inhibitor of Protein Kinase C (PKC) that exhibits concentration-dependent inhibition of QGY-7703 cell proliferation. As a natural product derived from Garcinia nervosa, it serves as a valuable tool in cancer research to explore PKC-related signaling pathways and its effects on tumor cell growth. Its unique properties make it suitable for studies aiming to elucidate the role of PKC in various cancer types. -
PKC Inhibitor
[Ala113]MBP(104-118) is a noncompetitive inhibitor of protein kinase C (PKC), demonstrating IC50 values between 28-62 μM. This peptide is crucial for studying the regulatory mechanisms of PKC in various biological contexts. Its inhibition of PKC activity makes it a valuable tool for investigating signal transduction pathways and their implications in disease states. Researchers can utilize this reagent to explore PKC's role in cellular processes, contributing to the understanding of therapeutic targets in cancer and other diseases. -
PTHR/PKCα/β Activator
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. -
Non-selective Protein Kinase Inhibitor
Staurosporine-Boc is a potent non-selective inhibitor of protein kinases, derived from the actinobacterium Streptomyces staurosporeus. This compound effectively inhibits a wide range of protein kinases, including protein kinase C (PKC), as well as tyrosine and serine/threonine kinases. Due to its broad activity profile, Staurosporine-Boc is extensively utilized in biological research, particularly in studies examining cell signaling pathways and related mechanisms. -
β1 PKC Fragment
Protein Kinase C (661-671) is a peptide fragment derived from the β1 isoform of protein kinase C (PKC). This fragment is crucial for studying the regulatory mechanisms of PKC in cellular growth control and its role in tumor promotion. It serves as an important tool for research into cancer biology and signaling pathways associated with PKC activity. -
Phorbol Ester
Sapintoxin A is a phorbol ester derived from the unripe fruits of Sapium indicum. This compound exhibits significant biological activity by acting on protein kinase C (PKC) pathways, making it valuable in the study of signal transduction and cancer research. Its applications include investigating the role of PKC in various cellular processes and understanding tumorigenesis mechanisms. -
PKC Pseudosubstrate Inhibitor
Protein Kinase C (19-35) Peptide serves as a pseudosubstrate inhibitor of Protein Kinase C (PKC). By potentially blocking the substrate-binding site within the kinase domain, this peptide renders the cytoplasmic form of PKC inactive. This inhibition is valuable for investigating PKC-related signaling pathways and understanding its role in various cellular processes. Its applications extend to research focused on cell proliferation, differentiation, and apoptosis associated with PKC activity. -
PKCδ Substrate
PKCδ Peptide Substrate is a highly specific substrate that targets the δ isoform of Protein Kinase C (PKCδ). Featuring the amino acid sequence corresponding to residues 422-443 of murine eEF-1α and incorporating Thr-431, this peptide supports detailed studies of PKCδ activity. It is suitable for a variety of research applications, including kinase assays and understanding PKCδ's role in cellular signaling pathways. -
aPKCζ inhibitor
aPKC-IN-1 is a selective inhibitor of atypical protein kinase C zeta (aPKCζ). This compound plays a crucial role in modulating cellular processes related to vascular permeability and inflammation. It is a valuable tool for investigating various disease mechanisms associated with these biological pathways, making it pertinent for research in areas such as cancer and autoimmune disorders.
