Catalog No.
Product Name
Application
Product Information
Citations
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PKCα Activator
12-Deoxyphorbol 13-isobutyrate is a potent activator of PKCα, derived from the latex of Euphorbia resinifera. It enhances the proliferation and activation of neural stem cells (NSCs) and promotes the release of TGFα, demonstrating a significant role in neurogenesis. Additionally, this compound has been shown to improve cognitive performance and hippocampal neurogenesis in senescence-accelerated mouse-prone (SAMP8) models, making it a valuable reagent for research into neurodegenerative diseases. -
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. -
Reaction substrate
KRAKAKTTKKR is a synthetic peptide that serves as a substrate for protein kinase C (PKC). It facilitates the study of PKC activity by enabling the assessment of phosphorylation processes. This peptide is utilized in biochemical assays to explore signaling pathways and cellular mechanisms involving PKC, contributing to research in cancer, diabetes, and other diseases influenced by this kinase. -
Antiarrhythmic Agent
HNS-32 is an antiarrhythmic agent that demonstrates vasodilatory effects, providing protective benefits against ischemic and reperfusion arrhythmias in canine hearts. This compound exhibits significant negative chronotropic effects on mammalian ventricular myocardium, highlighting its potential for applications in acute coronary syndrome research. HNS-32 serves as a valuable tool for exploring the mechanisms and treatment options for cardiac arrhythmias. -
Bioactive Peptide
PKCd (8-17) is a bioactive peptide derived from the V1 domain of protein kinase C (PKC)d. This peptide effectively inhibits phorbol 12-myristate 13-acetate (PMA)-induced PKCd translocation and activation. Its inhibitory effects on PKCd contribute to reduced ischemic damage in cardiac and cerebral cells, promote fibroblast proliferation, and inhibit graft coronary artery disease in murine models, making it valuable for research in cardiac and cerebrovascular conditions. -
PKA Substrate
Phosphate acceptor peptide is a specific substrate for cyclic AMP-dependent protein kinase (PKA), facilitating the study of phosphorylation processes. Additionally, it exhibits weak inhibitory activity against protein kinase C (PKC), making it useful in exploring the mechanisms of kinase signaling pathways. This reagent is applicable in various biochemical assays aimed at understanding cellular signaling and regulation. -
Anti-cancer Agent
Bryostatin 2 is a 20-membered ring lactone that acts as an anti-cancer agent, specifically targeting the protein kinase C (PKC) pathway. This compound has demonstrated potential in the research of P-388 lymphocytic leukemia, offering insights into its mechanisms and therapeutic applications. Bryostatin 2 is a valuable tool for investigating the role of PKC in cancer cell growth and survival. -
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. -
Stable Isotope
Stearoyl-L-carnitine-d9 chloride is a deuterated analogue of Stearoyl-L-carnitine chloride, classified as a stable isotope. It serves as a valuable tool in metabolic studies, particularly in understanding lipid metabolism and energy deficiency in type 2 diabetes models. This compound is known to inhibit protein kinase C (PKC) and lecithin cholesterol acyltransferase (LCAT), while also acting as a metabolomic biomarker for Parkinson's disease. Additionally, it demonstrates reduced potency as an inhibitor of GlyT2, providing insights into neurotransmitter dynamics. -
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. -
Phospholipid
Dioleyl phosphatidylserine is a phospholipid known for its role in membrane dynamics and cellular signaling. It has been shown to activate protein kinase C gamma (PKC-γ) at concentrations of 100 μM, particularly under calcium ion (Ca2+) levels less than 0.5 μM. This reagent is valuable for research in neuroscience and cellular biology, particularly in studies focusing on synaptic transmission and cellular responsiveness. -
Protein Kinase C Activator
Methyl arachidonate is an activator of protein kinase C, functioning as an orally active substrate that is subject to esterase-mediated hydrolysis. It promotes the indirect activation of protein kinase C through the generation of eicosanoid metabolites from the arachidonic acid metabolic pathway, demonstrating differential effects via cyclooxygenase products at low concentrations and lipoxygenase products at elevated concentrations. This compound is valuable for investigations into mechanisms related to lipodystrophy. -
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. -
Derivative of L-Tyrosine
3-Methyl-L-tyrosine is a derivative of L-Tyrosine that features a methyl group at the third position of the aromatic ring. This compound acts as a substrate for the protein tyrosine kinase Csk, demonstrating a catalytic efficiency (kcat/Km) of 38% relative to L-Tyrosine, indicating its role in modulating the enzymatic processing of Gsk. Research applications of 3-Methyl-L-tyrosine include studying the molecular recognition mechanisms of Gsk's substrates, which is essential for the design of specific inhibitors targeting Gsk in various therapeutic areas. -
Stable Isotope
Stearoyl-L-carnitine-d3 is a deuterated form of Stearoylcarnitine, functioning primarily as a stable isotope for research applications. This fatty ester lipid is an endogenous metabolite, known to inhibit protein kinase C (PKC) and accumulate in pancreatic β cells, resulting in impaired insulin synthesis and energy deficiency in type 2 diabetes models. Additionally, Stearoyl-L-carnitine-d3 inhibits lecithin cholesterol acyltransferase (LCAT) in animal plasma and serves as a potential metabolomics biomarker for Parkinson’s disease, further expanding its utility in metabolic research. -
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. -
PKC Activator
Farnesylthiotriazole (FTT) is a potent activator of protein kinase C (PKC), with a dissociation constant (Kd) of 0.8 μM. This compound plays a significant role in various signaling pathways, making it a valuable tool in cancer research. Its ability to modulate PKC activity can aid in the investigation of tumor biology and therapeutic strategies targeting PKC-related pathways. -
Diacylglycerol
1-Oleoyl-2-linoleoyl-sn-glycerol is a diacylglycerol that acts as an activator of protein kinase C (PKC). This activation initiates downstream signaling cascades that are vital in promoting tumor growth, making it a relevant compound for cancer research. Its role in the signaling pathways related to breast cancer highlights its potential use in studying tumorigenesis and therapeutic strategies. -
PKC Activator
1,2-Dipentadecanoyl-sn-glycero-3-phospho-(1'-rac-glycerol) sodium is a potent activator of the protein kinase C (PKC) family. This anionic phospholipid is integral to mitochondrial and microsomal membranes, significantly contributing to the composition and function of lung surfactant, particularly within lamellar body membranes in the lungs. Its unique properties make it a valuable tool for studying PKC-mediated signaling pathways and lung physiology. -
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. -
Stable Isotope
(±)-1,2-Diolein-CC3 is a stable isotope-labeled derivative of (±)-1,2-Diolein, also known as 1,2-Dioleoyl-rac-glycerol-13C3. This compound acts as an activator of protein kinase C (PKC) and is known to enhance calcium ion influx in myotubes. It is particularly useful in research applications studying lipid signaling pathways, cell proliferation, and muscle physiology. -
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. -
PKC Inhibitor
Bisindolylmaleimide X is a potent protein kinase C (PKC) inhibitor that exhibits cell-penetrating properties. It effectively inhibits the proliferation of CD4 T cells in vitro and shows antagonistic activity against cyclin-dependent kinase 2 (CDK2) with an IC50 of 200 nM. Additionally, Bisindolylmaleimide X suppresses eNOS-Ser1177 phosphorylation in human embryonic vein endothelial cells. This compound is valuable for studying mechanisms in the immune system and cardiovascular diseases. -
PKC Inhibitor
DL-erythro-Dihydrosphingosine is a sphingosine-derived protein kinase C (PKC) inhibitor that functions by directly inhibiting phospholipase A2 (PLA2) activity. This compound also attenuates the function of Bcl-2, a protein that plays a crucial role in regulating apoptosis. Additionally, DL-erythro-Dihydrosphingosine inhibits matrix metalloproteinases (MMPs), which are involved in various cellular processes. Its unique biological activity makes it valuable for research in cancer and inflammatory disease models. -
PKC Activator
1,2-Dimyristoyl-sn-glycerol is a saturated diacylglycerol that acts as a weak second messenger for the activation of Protein Kinase C (PKC). This compound is utilized in research applications to study PKC signaling pathways, which are crucial in various cellular processes including growth, differentiation, and apoptosis. As a PKC activator, it can help elucidate the role of PKC in different biological contexts and disease models. -
PKC/HCMV Inhibitor
Bisindolylmaleimide IV is a selective inhibitor of protein kinase C (PKC), exhibiting IC50 values between 0.1 and 0.55 μM. It also demonstrates inhibition of protein kinase A (PKA) with IC50 ranging from 3.1 to 11.8 μM. In addition to its kinase inhibitory properties, Bisindolylmaleimide IV effectively inhibits human cytomegalovirus (HCMV) replication in cell culture, displaying an IC50 of 0.2 μM. This reagent is valuable for research applications focused on signal transduction and viral pathogenesis. -
Myo1s/TGF-β Inhibitor
Pentachloropseudilin is a potent reversible allosteric inhibitor targeting Myo1s (class 1 myosins), exhibiting IC50 values ranging from 1 to 5 μM for mammalian class-1 myosins, while displaying greater than 90 μM for class-2 and class-5 myosins. Additionally, it effectively inhibits transforming growth factor-β (TGF-β) signaling, with an IC50 of 0.1 to 0.2 μM. This compound is valuable for research in cellular signaling pathways and myosin function, contributing to studies in cell motility and tissue remodeling. -
PKC Inhibitor
PKC-iota inhibitor 1 is an inhibitor of protein kinase C-iota (PKC-ι) with an IC50 value of 0.34 μM. This compound demonstrates significant biological activity relevant to cancer research, making it a valuable tool for investigating the role of PKC-ι in tumorigenesis and signal transduction pathways. It is suitable for studies focused on cancer biology and therapeutic interventions targeting PKC-ι. -
PKA Anchoring Inhibitor
st-Ht31 is a membrane-permeable peptide that inhibits protein kinase A (PKA) anchoring. It effectively induces cholesterol and phospholipid efflux and has been shown to completely reverse foam cell formation in macrophages. This compound offers valuable insights into PKA-related signaling pathways and metabolic health research. -
PKC Inhibitor
Sangivamycin is a nucleoside analog that serves as a potent inhibitor of protein kinase C (PKC) with a Ki value of 10 μM. This compound exhibits significant antiproliferative activity against a diverse range of human cancers, making it a valuable tool for cancer research and therapeutic studies focused on PKC modulation. Its targeted mechanism of action positions Sangivamycin as a promising candidate for further exploration in cancer treatment. -
Anti-CD73/TGF-β Antibody
Dalutrafusp alfa is a bifunctional antibody that targets CD73 and TGF-β, key components involved in the immunosuppressive pathway. This compound modulates immune responses by inhibiting adenosine production and blocking TGF-β signaling. It is primarily utilized in research focused on tumor immunology and the modulation of immune checkpoints. Its unique mechanism allows for exploration in various therapeutic applications, particularly in cancer treatment and autoimmune diseases. -
PKA Inhibitor
2'-Deoxy-NAD+ sodium is a sodium salt derivative of 2'-Deoxy-NAD+ that functions as a noncompetitive inhibitor of NAD+ with a Ki value of 32 μM. This reagent is valuable for investigating ADP-ribosyl transfer reactions, providing insights into cellular processes involving protein modification. It is particularly useful in studies related to protein kinase A (PKA) activity and regulatory mechanisms in biological systems. -
PKCζ/ι Pseudosubstrate Inhibitor
PKCζ/ι Pseudosubstrate Inhibitor serves as a specific inhibitor of protein kinase C (PKC) isoforms ζ and ι. This compound exhibits broad-spectrum inhibitory effects on the PKC enzyme family, making it valuable for studies investigating the role of PKC in cell signaling and neurobiology. Additionally, it has been shown to induce memory impairment, which may be relevant for research on cognitive function and associated disorders. -
ALK4/5/7 Inhibitor
A 83-01 sodium is a selective inhibitor of the transforming growth factor-beta (TGF-β) type I receptors ALK4, ALK5, and ALK7. With IC50 values of 12 nM, 45 nM, and 7.5 nM, it effectively blocks transcriptional activity induced by these kinases. This compound is valuable for research applications focused on TGF-β signaling pathways and regulation of cellular processes such as proliferation, differentiation, and epithelial-mesenchymal transition. -
ACVR2A-IgG Fc Fusion Protein
Sotatercept is a soluble activin receptor 2A (ACVR2A) IgG Fc fusion protein that modulates growth differentiation pathways by combining activin and growth differentiation factor signals. This compound has demonstrated potential biological activity in restoring the balance between growth promotion and inhibition, making it a promising candidate for research in pulmonary arterial hypertension, anemia, bone loss, erythropoiesis, and osteolytic lesions associated with multiple myeloma. Its function highlights its value in studying conditions related to dysregulated signaling pathways in these diseases. -
TGFbR1 Inhibitor
PF-06952229 is a potent and selective inhibitor of TGFbR1, demonstrating oral bioavailability. By specifically binding to TGFbR1, it effectively blocks TGFbR1-mediated signaling pathways. This compound shows significant promise as an antineoplastic agent, particularly in the study of solid tumors, including metastatic breast cancer. Its mechanism makes it a valuable tool for understanding TGFbR1's role in cancer progression and therapy. -
TGFβ1 Inhibitor
TGFβ1-IN-1 is a potent inhibitor of transforming growth factor-beta 1 (TGF-β1). This compound effectively inhibits the upregulation of fibrosis markers such as α-SMA and fibronectin, making it a valuable tool for investigating liver fibrosis and related pathologies. TGFβ1-IN-1 is suitable for research applications focused on fibrosis modulation and therapeutic interventions targeting TGF-β1 signaling pathways. -
BMPR2 Inhibitor
CDD-1653 is a potent and selective inhibitor of Bone Morphogenetic Protein Receptor 2 (BMPR2) with an IC50 of 2.8 nM. By diminishing ATP binding to the kinase domain of BMPR2, CDD-1653 modulates the phosphorylation of SMAD1/5/8 transcription factors, which are essential components of the BMP signaling pathway. This reagent is suitable for investigating diseases associated with dysregulation in the BMP signaling cascade. -
ALK5 Inhibitor
Vactosertib Hydrochloride is a potent inhibitor of activin receptor-like kinase 5 (ALK5), characterized by its ATP-competitive mechanism and an IC50 of 12.9 nM. Additionally, it demonstrates inhibitory effects on ALK2 and ALK4 with IC50 values of 17.3 nM. This compound exhibits significant antimetastatic activity and anticancer properties, making it a valuable research tool for studies related to cancer biology and therapeutic development targeting TGF-β signaling pathways. -
Bifunctional Fusion Protein
Bintrafusp alfa is a bifunctional fusion protein that consists of the extracellular domain of TGF-β receptor II fused to a human IgG1 monoclonal antibody, which inhibits programmed cell death ligand. This innovative reagent exhibits significant anti-tumor activity by modulating immune responses and transforming the tumor microenvironment. Bintrafusp alfa is primarily utilized in cancer research to explore its therapeutic potential and enhance understanding of immune evasion mechanisms in tumors. -
ALK5 Inhibitor
THRX-144644 is a selective ALK5 inhibitor with a very low IC50 value of 0.14 nM, demonstrating potent inhibition of the TGFβ signaling pathway. This compound is designed for lung-targeted applications, offering an alternative that minimizes systemic toxicities typically linked to broader TGFβ pathway inhibition. THRX-144644 is valuable for research projects focused on fibrosis, cancer biology, and respiratory diseases. -
TGF-β Inhibitor
Pentabromopseudilin (PBrP) is a potent inhibitor of transforming growth factor-β (TGF-β), functioning as a reversible allosteric modulator of myosin Va (MyoVa). Isolated from marine bacteria, PBrP displays significant antimicrobial, anti-tumor, and phytotoxic properties. This compound is valuable for research in fibrotic diseases and cancer, providing insight into TGF-β mediated pathways and their implications in disease progression. -
BMP Receptor Agonist
SY-LB-57 is a potent agonist of bone morphogenetic protein (BMP) receptors, facilitating BMP signaling pathways. This compound demonstrates significant biological activity in promoting bone formation and has potential applications in research related to osteogenesis, fracture healing, and pulmonary arterial hypertension. Its ability to enhance BMP signaling makes SY-LB-57 a valuable tool in the study of skeletal and vascular diseases. -
ALK5 Inhibitor
IN-1130 is a highly selective inhibitor of the transforming growth factor-β type I receptor kinase (ALK5), exhibiting an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. This compound also demonstrates inhibitory effects on ALK5 phosphorylation of casein with an IC50 of 36 nM and on p38α mitogen-activated protein kinase at an IC50 of 4.3 μM. IN-1130 is beneficial for research focused on renal fibrosis in obstructive nephropathy as well as the blockage of breast cancer lung metastasis, providing valuable insights into TGF-β signaling pathways. -
TGF-β Inhibitor
CJJ300 is a selective inhibitor of transforming growth factor-β (TGF-β), exhibiting an IC50 value of 5.3 µM. It effectively disrupts the formation of the TGF-β-TβR-I-TβR-II signaling complex, thereby inhibiting TGF-β signaling pathways. This compound is valuable for research applications focused on the modulation of TGF-β related processes, including fibrosis, cancer progression, and immune regulation. -
ALK5 Inhibitor
ALK5-IN-8 is a potent inhibitor of transforming growth factor beta receptor I (TGFβRI, also known as ALK5). This compound effectively blocks the phosphorylation of downstream signaling proteins such as Smad2 and Smad3 by preventing the binding of TGFβRI to its ligands, thereby disrupting TGF-β signaling pathways. ALK5-IN-8 is valuable for research into various diseases associated with ALK5-mediated signaling, contributing to the understanding of pathophysiological conditions influenced by TGF-β.
