Protein Kinase A (PKA)

Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent.

A-674563 is a B/Akt inhibitor with an IC50 of 14 nM and also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nM, respectively.

H 89 dihydrochloride is a cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase.

AT13148 is a novel oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity, which shows a distinct mechanism of action from other AKT inhibitors.

A-3 Hydrochloride is an inhibitor of PKA (cAMP-dependent protein kinase, Ki=4.3μM) and cGMP-dependent protein kinase, Ki=3.8μM, PKC (protein kinase C, Ki=47μM), casein kinase I and II, and MLCK (myosin light chain kinase) ( Ki=7.4μM).

MK-2 Inhibitor III (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM.

NH125 is a selective eEF-2 kinase inhibitor.

PKA inhibitor fragment (6-22) amide is a synthetic peptide that acts as a protein kinase inhibitor.

AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively, little activity outside the AGC kinase family.

KT 5720 is prepared by a modificiation of K-252a (sc-200517), which is synthesized by the fungus Nocardiopsis sp.

Rp-cAMPS is a cell-permeable and reversible inhibitor of PKA (protein kinase A) (Ki = 11 uM). Rp-cAMPS is resistant to hydrolysis by phosphodiesterases and is noncompetitive with respect to ATP.

PKI 14-22 amide, myristoylated is a useful heat stable cAMP-dependent protein kinase inhibitor. This is often used to study PKA in cellular systems in-vitro.

cGMP Dependent Kinase Inhibitor Peptid is a specific cGKI (cyclic GMP-dependent protein kinase) inhibitor. Data indicates that it does not block cyclic GMP-dependent protein kinase phosphorylation of intact histones and has been used to study Plasmodium falciparum.

CCG215022 is a potent GRK2 and GRK5 inhibitor. CCG215022 exhibited nanomolar IC50 values against both GRK2 and GRK5 and good selectivity against other closely related kinases such as GRK1 and PKA.

Warangalone is a prenylated isoflavone from the insecticidal plant Derris scandens that acts as a powerful inhibitor of protein kinase A.

HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50 = 8, 12, and 4 μM, respectively).

UCN-02 (7-epi-Hydroxystaurosporine) is a selective protein kinase C (PKC) inhibitor produced by Streptomyces strain N-12, with IC50s of 62 nM and 250 nM for PKC and protein kinase A (PKA), respectively.

BAMB-4(ITPKA-IN-C14) is a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A((ITPKA) with IC50 of 37 μM in ADP-Glo Assay.

MK2-IN-1 hydrochloride is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.

HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50s = 8, 12, and 4 ?M, respectively).

HA-1004 is a selective and multifunctional inhibitor of cyclic nucleotide-dependent protein kinases, including protein kinase A (PKA) and cyclic GMP-dependent protein kinase (PKG). It regulates key second messenger pathways involving cyclic AMP and cyclic GMP and has broad pharmacological effects. HA-1004 inhibits lipolysis and induces vascular smooth muscle relaxation, acting as a vasodilator. It also functions as a calcium antagonist, contributing to its ability to suppress contraction in rabbit aortic strips. In neurological models, HA-1004 has been shown to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models, suggesting potential relevance in addiction and neurochemical regulation. Its diverse actions make it a valuable tool for studying cardiovascular, metabolic, and neurobiological processes.

Akt1&PKA-IN-2 (Compound R-29) is a AKT1 and PKA inhibitor with selectivity for CDK2, with IC50 values of 0.007 and 0.01 μM, respectively. Akt1&PKA-IN-2 is applicable for cancer research.

Akt1&PKA-IN-1 is a potent dual inhibitor targeting both Akt and Protein Kinase A (PKA), exhibiting IC50 values of 0.03 μM for PKAα and 0.11 μM for Akt, with a higher IC50 of 9.8 μM for cyclin-dependent kinase 2 (CDK2). This compound demonstrates selective inhibition of CDK2, making it a valuable tool for research in cancer biology and cellular signaling pathways. Akt1&PKA-IN-1 is useful for studying the regulatory role of these kinases in cellular processes and potential therapeutic applications.

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.

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.

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.

HA-1004 hydrochloride is a selective inhibitor of protein kinase A (PKA), known for its ability to inhibit lipolysis and promote vascular relaxation. In addition to its PKA inhibition, HA-1004 also functions as a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein synthesis, impacting smooth muscle and second messenger pathways. This compound serves as a vasodilator, effective in inhibiting the contraction of rabbit aortic strips, and can also antagonize ERK and tyrosine hydroxylase phosphorylation in morphine abstinence models.

HA-1004 dihydrochloride is a selective inhibitor of protein kinase A (PKA), demonstrating significant inhibition of lipolysis and induction of vascular relaxation. Additionally, it acts as a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein kinase, playing a crucial role in regulating smooth muscle activity and second messenger pathways. This compound serves as a vasodilator, effectively inhibiting contraction in rabbit aortic strips, and also antagonizes ERK and tyrosine hydroxylase phosphorylation in models of morphine abstinence.

LX7101 monohydrochloride is a potent inhibitor of LIM-kinase, ROCK, and PKA, exhibiting IC50 values of 24 nM, 1.6 nM, 10 nM, and <1 nM for LIMK1, LIMK2, ROCK2, and PKA, respectively. This compound demonstrates significant selectivity for LIMK2 with an IC50 of 4.3 nM in contrast to 32 nM for LIMK1 at 2 μM ATP. LX7101 monohydrochloride is valuable for research into ocular hypertension and associated glaucoma, providing insights into potential therapeutic strategies targeting these pathways.

MDL 27032 is a selective active site-directed inhibitor of protein kinase C (PKC) and cAMP-dependent protein kinase (PKA), exhibiting Ki values of 24 μM and 14.3 μM, respectively. This compound demonstrates significant vasodilatory effects by relaxing vascular smooth muscle. Its properties make MDL 27032 a valuable tool for investigating PKC and PKA-mediated pathways in cardiovascular research and other related studies.

Rp-8-Br-cAMPS sodium is a selective inhibitor of Protein Kinase A (PKA) that functions by occupying the cAMP binding sites on the regulatory subunits of PKA type I. This prevents the dissociation and activation of PKA, making it a valuable tool for studying signaling pathways dependent on PKA. Research applications include investigations into tumor biology, retrovirus-induced immune deficiencies, and the regulation of insulin secretion.

H-8 dihydrochloride is a reversible, cell-permeable inhibitor of protein kinase A (PKA) that operates through an ATP-competitive mechanism. It effectively modulates PKA activity, making it a valuable tool for investigating cellular signaling pathways. This compound is widely utilized in cancer research and studies focused on metabolic disorders, allowing researchers to elucidate the roles of PKA in various biological contexts.

PKI (14-24)amide TFA is a potent inhibitor of protein kinase A (PKA) that effectively blocks cyclic AMP-dependent protein kinase activity in various cellular contexts. This compound demonstrates significant inhibitory action, making it valuable for studies involving PKA-related signaling pathways. Its utilization in research can provide insights into the molecular mechanisms of PKA-mediated processes in health and disease.

PKI (14-24)amide is a potent inhibitor of Protein Kinase A (PKA), effectively disrupting the activity of cyclic AMP-dependent protein kinase. This compound has been shown to strongly inhibit PKA activity in cell homogenates, making it a valuable tool for studying PKA-related signaling pathways and their biological implications. Its application in research can facilitate investigations into cellular processes regulated by PKA, contributing to a better understanding of various physiological and pathological conditions.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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-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.

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-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.

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.

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.