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Catalog No.
Product Name
Application
Product Information
Citations
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PKA Inhibitor
H-9 Dihydrochloride is a potent inhibitor of protein kinase A (PKA), effectively modulating signaling pathways involved in various biological functions. At a concentration of 10 μM, it significantly diminishes the excitatory response to 5-hydroxytryptamine (5-HT) and exhibits direct effects on pharyngeal activity. Additionally, H-9 Dihydrochloride inhibits signal transduction and cell growth in epidermal growth factor (EGF)-dependent epithelial cell lines, making it a valuable tool for research in cellular signaling and growth regulation. -
ROCK/NET Inhibitor
Netarsudil hydrochloride is a selective inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). It effectively lowers intraocular pressure by promoting relaxation of trabecular meshwork cells and dilation of episcleral veins, enhancing aqueous humor outflow while simultaneously reducing its production. This compound is primarily utilized in research related to ocular hypertension and primary open-angle glaucoma. -
PKA Inhibitor
Metadoxine is a potent inhibitor of protein kinase A (PKA), specifically disrupting the PKA-cAMP response element binding protein (CREB) pathway. This compound is effective in blocking adipocyte differentiation, making it valuable for research into metabolic disorders and obesity-related pathways. Its ability to modulate PKA activity demonstrates potential applications in studying cellular signaling and metabolic regulation. -
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. -
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. -
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 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 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 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. -
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 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. -
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. -
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. -
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 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. -
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. -
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 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. -
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. -
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 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. -
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. -
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. -
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. -
PKC Inhibitor
ICP-103 is a highly selective protein kinase C (PKC) inhibitor with an IC50 of 30 nM. This compound has demonstrated potent inhibitory activity against PKC, making it a valuable tool for cancer research. ICP-103 can be utilized to explore the role of PKC in tumorigenesis and therapeutic resistance, contributing to a deeper understanding of potential cancer treatment strategies. -
Inhibitor Peptide
pep2-EVKI (YNVYGIEEVKI) is an inhibitor peptide that selectively targets and disrupts the interactions of Protein Interacting with C kinase 1 (PICK1). This compound is known to exert opposing effects on synaptic α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) function relative to PICK1 expression. It serves as a valuable tool for studying synaptic signaling pathways and understanding the role of PICK1 in synaptic plasticity and related neurobiological processes. -
PKC Inhibitor
7-Oxostaurosporine is a selective inhibitor of protein kinase C (PKC), demonstrating significant efficacy in inhibiting tumor proliferation. This compound induces apoptosis in cancer cells and effectively disrupts the nuclear factor (NF)-κB/p-p65 signaling pathway, making it valuable for cancer research and therapeutic studies focused on PKC-related pathways. Its potent biological activity highlights its potential utility in understanding tumor biology and developing targeted cancer therapies. -
PKC Inhibitor
[Ala107]MBP(104-118) is a noncompetitive inhibitor of protein kinase C (PKC), exhibiting IC50 values between 46-145 μM. This peptide is utilized in research to study PKC activity and its role in cellular signaling pathways. Its ability to selectively inhibit PKC makes it a valuable tool in investigating the implications of PKC in various disease states and pharmacological interventions. -
PKC Inhibitor
K-252b is an indolocarbazole that acts as a selective protein kinase C (PKC) inhibitor. Its primary mechanism involves the inhibition of PKC enzymes, essential for various cellular signaling pathways. K-252b is particularly useful in studies assessing the role of PKC in phosphorylation processes and can be applied in cell culture to investigate the effects of targeted PKC modulation on cellular functions. However, its limited membrane permeability necessitates specific experimental conditions for effective use.
