Catalog No.
Product Name
Application
Product Information
Citations
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PKC activating agent
Decursinol angelate, a cytotoxic and protein kinase C (PKC) activating agent from the root of Angelica gigas, possesses anti-tumor and anti-inflammatory activities. -
PKC inhibitor
Iso-H7 dihydrochloride is an inhibitor of phosphokinase C. - Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.
- 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.
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PKC isoenzymes inhibitor
CRT0066854 is a potent and selective inhibitor of atypical protein kinase C (PKC) isoenzymes. It inhibits full-length PKCι, PKCζ, and ROCK-II with IC₅₀ values of 132 nM, 639 nM, and 620 nM, respectively. - Gondoic acid (cis-11-Eicosenoic acid) is a monounsaturated long-chain fatty acid found in various plant oils and nuts. It exhibits anti-inflammatory activity by reducing reactive oxygen species (ROS) production and inhibiting the PKCθ/ERK/STAT3 signaling pathway. Gondoic acid is also utilized as a raw material in medical applications and as a moisturizing agent in cosmetic formulations.
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GPR55 antagonist
ML192 is a selective antagonist of G protein-coupled receptor 55 (GPR55), effectively inhibiting GPR55-mediated signaling pathways. It blocks β-arrestin trafficking, suppresses ERK1/2 phosphorylation, and prevents PKCβII translocation, thereby interfering with downstream cellular responses. ML192 is a valuable tool for studying the physiological and pathological roles of GPR55 in processes such as inflammation, pain, cancer, and metabolic regulation. -
PKCβ Inhibitor
PKCβ Inhibitor 1 is a highly selective, ATP-competitive inhibitor targeting protein kinase C beta (PKCβ) with IC50 values of 21 nM for PKCβ1 and 5 nM for PKCβ2. This compound demonstrates over 60-fold selectivity for PKCβ2 compared to other PKC isozymes such as PKCα, PKCγ, and PKCε. It is a valuable tool for investigating the roles of PKCβ in various signaling pathways and its implications in diseases such as cancer and diabetes. -
p-Ezrin Inhibitor
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. -
DGK/PKC Inhibitor
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. -
PKN1/2 Inhibitor
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. -
Drug Analog
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. -
PKC-θ Inhibitor
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. -
Cytotoxic Lipid
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. -
PKMζ Inhibitor
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. -
PKC Inhibitor
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. -
PKC Substrate
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. -
PKC Inhibitor
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. -
PKC Activator
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. -
PKC Inhibitor
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. -
PKC Activator
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. -
PKC Inhibitor
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. -
PKCι Inhibitor
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. -
PKC Inhibitor
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. -
PKC Inhibitor
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. -
PKC-α Inhibitor
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. -
PKC Inhibitor
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. -
ATF2 Inhibitor
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. -
Protein C Substrate
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. -
Autoantigen Peptide
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). -
AQP1 Inhibitor
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. -
Protein Kinase Inhibitor
Protein Kinase Inhibitor 9 is a potent inhibitor of serine/threonine and tyrosine kinase activity. It demonstrates significant anti-proliferative effects, making it valuable for cancer research and the study of hyperproliferative disorders. Additionally, this compound can be applied in investigations related to rheumatoid arthritis, immune system dysfunctions, transplant rejections, and inflammatory disorders. -
PKCα Inhibitor
Bisindolylmaleimide III is a selective inhibitor of protein kinase C alpha (PKCα), effectively disrupting its activity. This compound selectively engages with PKCα or ribosomal S6 protein kinase 1 following their activation, making it a valuable tool in dissecting PKC-related signaling pathways. It is widely utilized in cancer research and studies investigating cell growth and differentiation. -
PKCθ Inhibitor
PKCTheta-IN-2 is a highly potent and selective inhibitor of protein kinase C theta (PKCθ) with an IC50 value of 0.25 nM. This compound demonstrates exceptional selectivity for PKCθ over more than 30 other kinases within the PKC subfamily. PKCTheta-IN-2 effectively inhibits interleukin-2 (IL-2) production in murine models, exhibiting an IC50 of 682 nM. Its use in research is particularly relevant for studies involving T cell signaling and autoimmune disorders. -
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.
