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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
PKC Inhibitor
N-Myristoyl-Lys-Arg-Thr-Leu-Arg is a selective inhibitor of protein kinase C (PKC), exhibiting an IC50 of 75 μM. This compound effectively inhibits the induction of the IL-2 receptor and production of IL-2 in the Jurkat human leukemic cell line. It can be utilized in research focused on understanding PKC-related signaling pathways and their role in immune responses. -
PKC-θ Inhibitor
PKC-theta inhibitor 2 hydrochloride is a highly selective inhibitor of protein kinase C theta (PKC-θ), exhibiting an IC50 of 18 nM. This compound modulates key signaling pathways associated with T cell activation and proliferation. It serves as a valuable tool in research investigating autoimmune diseases, cancer therapeutics, and immune response modulation. -
PKC Inhibitor
Safingol is a lyso-sphingolipid that acts as a selective protein kinase C (PKC) inhibitor. It has demonstrated potential in modulating various cellular signaling pathways, making it an important tool in cancer research and studies of cell survival and apoptosis. Safingol is valuable for investigating the role of PKC in diseases and may aid in the development of therapeutic strategies targeting this kinase. -
OPN4 Inhibitor
AE 51310 is an inhibitor of the OPN4 receptor, effectively disrupting the activation of protein kinase C (PKC) and the downstream BRAF/MEK/ERK signaling cascade. This compound is valuable for cancer research, particularly in the study of non-small cell lung cancer (NSCLC). Its ability to modulate critical signaling pathways makes AE 51310 a useful tool in investigating tumor biology and potential therapeutic targets. -
PKC-ι Inhibitor
PKCiota-IN-1 is a potent inhibitor of protein kinase C iota (PKC-ι) with an IC50 of 2.7 nM. This compound also exhibits inhibitory activity against PKC-α and PKC-ε, with IC50 values of 45 nM and 450 nM, respectively. PKCiota-IN-1 is valuable for studying the role of PKC-ι in various biological processes and has potential applications in cancer research and therapeutic strategies targeting PKC pathways. -
PKC Inhibitor
CIDD-0072424 is a selective inhibitor of Protein Kinase C-epsilon (PKCε), exhibiting an inhibitory constant (Ki) of 54 nM. This compound has been shown to reduce ethanol consumption and preference in a dose-dependent manner, making it a valuable tool for studying alcohol-related behaviors and signaling pathways. It is applicable in research investigating the role of PKCε in addiction and other neurobiological processes. -
PKC Inhibitor
MT477 is a potent protein kinase C (PKC) inhibitor that induces both apoptosis and necrosis in target cells. This compound effectively reduces the protein expression levels of Ras-GTP, p-Erk1/2, and p-Elk1. Due to its mechanism of action, MT477 demonstrates significant antitumor activity, making it a valuable tool for cancer research and therapeutic investigations. -
PKC Inhibitor
PKC-IN-5, a protein kinase C (PKC) inhibitor, disrupts the interaction between PKC epsilon (PKCe) and its adaptor protein RACK2. This inhibition can modulate PKC-mediated signaling pathways, making PKC-IN-5 a valuable tool for studying PKC-related cellular processes. Its application extends to research in cancer biology and neurodegenerative diseases, where PKC signaling plays a critical role. -
Protein Kinase C Inhibitor
Ro 31-8830 is a potent and selective inhibitor of protein kinase C, which plays a crucial role in various cell signaling pathways. This compound demonstrates anti-inflammatory activity and is valuable for research focused on inflammatory disorders. Its capabilities make Ro 31-8830 a significant tool for investigating the mechanisms underlying inflammation and evaluating potential therapeutic strategies. -
PKC Inhibitor
R8605 is a protein kinase C (PKC) inhibitor with a reported IC50 of 65 μM in the rat brain. This compound also inhibits calcium/phospholipid-independent phosphorylation of protamine, with IC50 values of 70 μM and 100 μM, respectively. R8605 is applicable in cancer research, facilitating studies on PKC-mediated signaling pathways and their implications in tumorigenesis. -
PKC Inhibitor
Safingol hydrochloride is a lyso-sphingolipid that functions as a potent inhibitor of protein kinase C (PKC). This compound exhibits significant biological activity in modulating cellular signaling pathways associated with cancer progression and apoptosis. Safingol hydrochloride is primarily utilized in research focused on cancer biology, cardiovascular disease, and neuroprotection, providing valuable insights into PKC-related mechanisms. -
PKCβII Inhibitor
PKCβII Peptide Inhibitor I is a selective inhibitor of Protein Kinase C beta II (PKCβII). This peptide demonstrates significant cardioprotective effects in rat models of ischemia/reperfusion injury, making it a valuable tool in cardiovascular research. Additionally, it has been shown to prevent vascular endothelial dysfunction, highlighting its potential applications in studying vascular health and related pathologies. -
Protein Kinase C Inhibitor/LTD4 Antagonist
LY 170198 is a potent protein kinase C inhibitor and LTD4 antagonist. This compound exhibits significant biological activity relevant to studies on tumor promotion, oncogene activation, and protein phosphorylation. Additionally, it is valuable for investigating feedback mechanisms in signal transduction pathways and cellular responses to growth factors, making it a useful tool for cancer research and related fields. -
PKC Inhibitor
Go 7874 is a protein kinase C (PKC) inhibitor that exhibits neuroprotective effects in models of immune-mediated neurotoxicity. This compound mitigates LPS/IFNg-induced neuronal cell death not through conventional PKC inhibition, but by suppressing the expression of inducible nitric oxide synthase (iNOS), leading to decreased nitric oxide (NO) production. Its unique mechanism makes Go 7874 a valuable tool for studying neuroprotective strategies in inflammatory conditions. -
PKCα Inhibitor
Desmethylglycitein (4',6,7-Trihydroxyisoflavone) is an inhibitor of protein kinase C (PKC)α, demonstrating significant anti-cancer and antioxidant activities. It directly binds to CDK1 and CDK2, leading to the suppression of their activity. Additionally, Desmethylglycitein inhibits PI3K in an ATP-competitive manner, affecting downstream signaling pathways and reducing adipogenesis in 3T3-L1 preadipocytes. Its mechanisms make it a valuable tool for research in cancer biology and metabolic disorders.
