Catalog No.
Product Name
Application
Product Information
Citations
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PKA Activator
Sp-8-CPT-cAMPS is a potent and selective activator of cAMP-dependent protein kinase A (PKA), specifically targeting PKA I and PKA II. This cAMP analog demonstrates a remarkable 153-fold selectivity for Site A of RI over Site A of RII and a 59-fold selectivity for Site B of RII over Site B of RI. Its ability to effectively modulate PKA activity makes it a valuable tool for research in signaling pathways and cellular responses associated with cAMP. -
PKA Substrate
H1-7 is a synthetic polypeptide designed as a substrate for protein kinase A (PKA). This compound effectively mimics histone H1 phosphorylation sites, allowing for the study of PKA-mediated phosphorylation processes. Its application is significant in understanding PKA signaling pathways and epigenetic modifications associated with histones in various biological contexts. -
PKA Antagonist
Rp-8-CPT-cAMPS is a potent antagonist of cAMP-dependent protein kinase A (PKA), inhibiting the activation of both PKA I and II. This cAMP analog selectively targets site A of the regulatory subunit type I over site A of type II, as well as site B of type II over site B of type I. Its ability to modulate PKA activity makes it a valuable tool for investigating downstream signaling pathways influenced by cAMP. Researchers can utilize Rp-8-CPT-cAMPS in studies focused on cellular responses and signal transduction mechanisms. -
PKA Inhibitor
GEM-231 is an 18mer antisense oligonucleotide that specifically targets the mRNA of the PKA-I (RIα regulatory subunit of cAMP-dependent protein kinase type I). This compound has demonstrated the ability to induce cell growth arrest, apoptosis, and differentiation across various cancer cell lines in vitro, as well as in tumor models in vivo. GEM-231 serves as a valuable tool for investigating PKA signaling pathways and their implications in cancer biology. -
PKA Agonist
8-Br-cAMP-AM is a cyclic adenosine monophosphate (cAMP) analog that functions as a protein kinase A (PKA) agonist. By mimicking cAMP, it activates critical signaling pathways such as PKA and Epac, facilitating studies on heart-related conditions. This compound is particularly useful for investigating cardiac ischemia and reperfusion injury, providing valuable insights into these pathological processes. -
PKA Inhibitor
PKI (5-24), amide is a potent inhibitor of cAMP-dependent protein kinase A (PKA), derived from the active region of the heat-stable inhibitor protein. With an inhibition constant (Ki) of 2.3 nM, it effectively disrupts PKA signaling pathways. This reagent is valuable for research applications focusing on PKA-mediated cellular functions and signaling cascades in various biological contexts. -
J-PKA Inhibitor
Aplithianines A is a selective inhibitor of J-PKAcα, exhibiting an IC50 value of 1 μM, while also demonstrating inhibition of wild-type PKA with an IC50 of 84 nM. This compound exerts its inhibitory effects by competitively binding to the ATP pocket of J-PKAcα, thereby affecting its catalytic activity. Aplithianines A is valuable for research applications involving protein kinase signaling pathways and the study of PKA-related cellular processes. -
PKA Inhibitor
PKItide is a potent inhibitor of Protein Kinase A (PKA), exhibiting an IC50 of 0.2 μM for cAMP-dependent PKA. This compound effectively disrupts PKA signaling pathways, making it a valuable tool for studying cellular processes regulated by cAMP. Research applications include investigating the role of PKA in various physiological and pathological conditions, as well as exploring therapeutic strategies targeting PKA-related diseases. -
PKA Activator
8-CPT-6-Phe-cAMP is a potent activator of protein kinase A (PKA), functioning as an analogue of the signaling molecule cyclic adenosine monophosphate (cAMP). This compound is widely utilized in research to study PKA-mediated pathways and cellular responses related to various physiological processes. Its ability to effectively modulate PKA activity makes it an essential tool for investigating signal transduction mechanisms and pharmacological interventions. -
PKA I/II Antagonist
Rp-cAMPS is a potent antagonist of cyclic adenosine monophosphate (cAMP) that effectively inhibits the activation of protein kinase A (PKA) types I and II, exhibiting Ki values of 12.5 µM and 4.5 µM, respectively. This cAMP analog is resistant to hydrolysis by phosphodiesterases, making it suitable for research focused on cAMP signaling pathways. Rp-cAMPS is commonly used in studies investigating the regulatory role of PKA in various physiological processes and disease models. -
PKA Inhibitor
Rp-8-Br-cAMPS is a potent inhibitor of protein kinase A (PKA) that functions by occupying the cAMP binding sites on the regulatory subunits of PKA type I. This inhibition prevents the dissociation and activation of PKA, thereby modulating downstream signaling pathways. Rp-8-Br-cAMPS is particularly useful in research applications focused on tumor biology, retrovirus-induced immune deficiency, and the regulation of insulin secretion. -
PKA Substrate
PKA Substrate is a selective peptide designed for the measurement of protein kinase A (PKA) activity. This substrate undergoes phosphorylation in the presence of active PKA, allowing for the detection and quantification of kinase activity in various biological samples. Its utility in biochemical assays makes it an essential tool for researchers investigating PKA-mediated signaling pathways. -
PKA Inhibitor
GSK466317A is a potent protein kinase A (PKA) inhibitor, exhibiting an IC50 of 12.59 μM. In addition to its primary target, GSK466317A also demonstrates inhibitory activity against GRK1, GRK2, and GRK5, with corresponding IC50 values of 1000 μM, 31.62 μM, and 39.81 μM, respectively. This compound is valuable for research applications involving signal transduction pathways and the study of G protein-coupled receptor (GPCR) functionality. -
PKA/PKC Inhibitor
Protein Kinase Inhibitor 7 is an inhibitor of Protein Kinase A (PKA) and Protein Kinase C (PKC). This compound modulates the autocrine motility factor (AMF) signaling pathway, demonstrating potential applications in cancer research and studies involving cell signaling without influencing overall cell motility. It is a valuable tool for elucidating the roles of PKA and PKC in various biological processes. -
MLCK/PKA Inhibitor
ME 3407 is a myosin light chain kinase (MLCK) and protein kinase A (PKA) inhibitor that disrupts H+-K+-ATPase redistribution. This compound effectively blocks gastric acid secretion and inhibits aminopyrine accumulation by preventing the microsomal-to-apical membrane redistribution of H+-K+-ATPase. ME 3407 demonstrates potential for use in research related to peptic ulcers and other gastrointestinal disorders. -
PKA Activator
Sp-cAMPS-AM is a cell-permeable analog of cyclic AMP (cAMP) that functions as a potent activator of Protein Kinase A (PKA). Upon cellular uptake, it releases its parent compound, Sp-cAMPS, which subsequently promotes PKA activation and CREB phosphorylation. This reagent is valuable for research applications in signaling pathways involving cAMP and PKA, facilitating studies on gene expression and cellular response mechanisms. -
PKG/PKA Activator
Sp-8-pCPT-cGMPS is a potent activator of protein kinase G (PKG) and protein kinase A (PKA) with significant cell membrane permeability and phosphodiesterase stability. This cyclic guanosine monophosphate analog effectively engages PKG types I α, I β, and II, making it invaluable for research in signal transduction pathways. It is utilized to investigate the role of cGMP in neural plasticity, synaptic transmission, and other physiological processes influenced by these kinases. -
AKAP-PKA interaction inhibitor
FMP-API-1 is an inhibitor of the A-kinase anchoring protein (AKAP)-PKA interaction. By binding to the allosteric site of protein kinase A (PKA) regulatory subunits, FMP-API-1 enhances PKA activity and promotes the function of aquaporin-2 (AQP2) in PKA-knockout renal cortical collecting duct cell lines (mpkCCD cells). This compound is valuable for investigating nephrogenic diabetes insipidus (NDI) and the underlying mechanisms of renal water transport. -
PKA Agonist
8-MA-cAMP (8-Methylamino-cAMP) is a cyclic AMP analog that serves as a selective agonist for protein kinase A (PKA), specifically targeting the B site of both type I and type II PKA. This compound demonstrates key biological activity by effectively modulating PKA-mediated signaling pathways. Researchers utilize 8-MA-cAMP in combination with priming analogs, such as 8-piperidinyl cAMP, to achieve precise activation of type I PKA, making it valuable for studies in cellular signaling and related therapeutic research. -
PKA Activator
Sp-6-Phe-cAMPS is a potent, selective activator of cAMP-dependent protein kinase (PKA) that exhibits membrane permeability. This compound uniquely does not directly activate exchange factors that are normally stimulated by cAMP, serving as a useful negative control for Epac studies. Sp-6-Phe-cAMPS is valuable in research focusing on neurodegenerative diseases, facilitating investigations into PKA signaling pathways and their implications in these conditions. -
PKA Activator
6-Bn-cAMP is a potent site-selective activator of cAMP-dependent protein kinase (PKA), specifically designed not to activate Epac. This compound demonstrates enhanced hydrolytic stability against phosphodiesterases, esterases, and amidases, along with significantly improved membrane permeability compared to standard cAMP. It is widely utilized in research applications aimed at elucidating PKA signaling pathways and their biological implications. -
PKA Activator
6-Phe-cAMP is a potent and membrane-permeant activator of protein kinase A (PKA), specifically targeting site A of both PKA isozymes. This compound demonstrates strong selectivity, making it an invaluable tool for studying PKA-mediated signaling pathways. Additionally, 6-Phe-cAMP is amenable to phosphorothioate modification, facilitating further research applications in cellular and molecular biology. -
PKC/PKA Inhibitor
Balanol is a highly selective ATP-competitive inhibitor of Protein Kinase C (PKC) and Protein Kinase A (PKA), demonstrating potent activity against various human PKC isozymes, including α, β-I, β-II, γ, δ, ε, η, and ζ, with IC50 values ranging from 4 to 150 nM. This compound effectively inhibits the phosphorylation of key downstream targets such as cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides, making it a valuable tool for research involving PKC/PKA signaling pathways. -
PKA/AKAP Inhibitor
PKA/AKAP-IN-2 is a non-peptide inhibitor targeting the interaction between protein kinase A (PKA) and A kinase anchoring proteins (AKAP). This compound disrupts the PKA-AKAP binding, providing valuable insights into signaling pathways influenced by cAMP. PKA/AKAP-IN-2 is useful for research into diseases linked to cAMP dysregulation and the broader implications of PKA signaling in cellular processes. -
PKA Inhibitor
4-Cyano-3-methylisoquinoline is a potent protein kinase A (PKA) inhibitor, exhibiting an IC50 at the micromolar range. This compound has demonstrated the ability to reverse morphine tolerance in murine models, highlighting its potential use in pain management research and studies exploring opioid signaling pathways. Its role as a PKA inhibitor makes it a valuable tool for investigating cellular processes regulated by this important kinase. -
PKA/AKAP Inhibitor
PKA/AKAP-IN-1 is a potent non-peptide inhibitor that selectively disrupts the interaction between protein kinase A (PKA) and A-kinase anchoring proteins (AKAP). This compound is valuable for investigating the role of cAMP signaling in various pathological conditions associated with its dysregulation. Research applications include studies on cellular signaling pathways and potential therapeutic interventions in diseases linked to altered PKA/AKAP interactions. -
PKA Agonist
8-OH-cAMP (8-Hydroxy-cAMP) is a polar, membrane-impermeable analog of cyclic adenosine monophosphate (cAMP) that selectively activates protein kinase A (PKA) while resisting degradation by cyclic nucleotide-dependent phosphodiesterases. This compound serves as a valuable tool for investigating the role of cAMP signaling in various biological processes, particularly in cardiovascular and metabolic disease research. Its unique properties enable researchers to elucidate PKA-mediated pathways and their implications in disease development. -
PKA Agonist
Sp-8-Br-cAMPS is a synthetic analog of cyclic adenosine monophosphate (cAMP) and serves as a potent agonist for protein kinase A (PKA) with an EC50 of 360 nM. This compound effectively activates PKA and has been shown to inhibit T cell proliferation and modulate the hemocyte non-self response in Lepidoptera larvae. Its significant biological activity makes it a valuable tool for research into PKA-mediated signaling pathways and immune responses. -
ROCK2 Inhibitor
ROCK2-IN-12 is a selective ROCK2 inhibitor, demonstrating an IC50 of 7.0 nM for ROCK2 relative to ROCK1. This compound exhibits potent antifibrotic effects by modulating the TGF-β/Smad and ROCK2/STAT3 signaling pathways, effectively reducing collagen deposition and reversing fibrosis in Bleomycin-induced pulmonary fibrosis mouse models. ROCK2-IN-12 is suitable for investigating lung diseases, particularly pulmonary fibrosis. -
ROCK2 Inhibitor
ROCK2-IN-7 is a selective inhibitor of the Rho-associated protein kinase 2 (ROCK2). It effectively disrupts ROCK2/pSTAT3 signaling pathways, leading to decreased systemic immune activation and reduced inflammation. This compound is particularly valuable in studies related to autoimmune conditions, such as psoriasis, as it provides insights into the modulation of immune responses and inflammatory processes. -
PKA Activator
8-Benzylthio-cAMP is a selective activator of cAMP-dependent protein kinases (PKA) that serves as a stable derivative of cyclic adenosine monophosphate (cAMP). Its increased resistance to phosphodiesterase hydrolysis and enhanced membrane permeability make it an effective tool for probing cAMP signaling pathways. This compound is widely used in research to investigate the regulatory roles of cAMP in cellular processes such as proliferation, differentiation, and apoptosis. -
Smad Inhibitor
(14S,15R)-14-Deoxyoxacyclododecindione is a selective inhibitor of the TGF-β-dependent Smad2/3 and IL-4-dependent STAT6 signaling pathways, exhibiting IC50 values of 90 nM and 20 nM, respectively. This compound has significant potential for applications in cancer research and the study of fibrotic diseases by modulating key signaling events. Its ability to inhibit these pathways makes it a valuable tool for investigating the role of TGF-β and IL-4 in various biological processes. -
TGF-β Inhibitor
TGF-βRI inhibitor 3 is a selective inhibitor of the TGF-β receptor type I (ALK5), designed to effectively disrupt TGF-β signaling pathways. It demonstrates notable inhibitory activity with IC50 values of 0.63 μM against ALK5 and 13 μM against c-Src kinase. This compound is valuable for research applications targeting fibrosis, cancer progression, and other TGF-β-mediated biological processes. -
TGF-beta/Smad Inhibitor
RepSox hydrochloride is a highly selective inhibitor of transforming growth factor-β receptor I (TGF-β-RI) and activin-like kinase 5 (ALK5). It effectively inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. This reagent is valuable for investigating the roles of TGF-β signaling in obesity and metabolic disorders, including type 2 diabetes. -
MAPKAPK2 Inhibitor
MK2-IN-1 is a selective inhibitor of MAPKAPK2 (MK2), exhibiting an IC50 of 0.11 µM. This compound significantly interferes with the phosphorylation of serine residues in Tfcp2l1, with an EC50 of 0.35 µM for phosphorylated HSP27. MK2-IN-1 serves as a valuable tool for studying the role of MK2 in cellular signaling pathways and its implications in various biological processes. -
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.
