pka in 1

PKA-IN-1 is a selective and potent cyclic AMP-dependent protein kinase (PKA) catalytic subunit (cAK) inhibitor (IC50: 0.03 μM).PKA-IN-1 can be used to study diseases of the immune system.

Akt1&PKA-IN-1 is a potent dual inhibitor of Akt and PKA, with IC50 values of 0.11 μM for Akt, 0.03 μM for PKAα, and 9.8 μM for CDK2, demonstrating selective inhibition of cyclin-dependent kinase 2 (CDK2).

Phanginin A, a natural product discovered in Caesalpinia sappan Linn, activates SIK1 and inhibits gluconeogenesis in mouse primary hepatocytes. Phanginin A increases PDE4 activity and suppresses the hepatic cAMP/PKA/CREB pathway, improving metabolic disorders in ob/ob mice. It may be used in studies of type 2 diabetes.

API-1 (NSC-177223) is a potent inhibitor of Akt. It induces GSK3-dependent, β-TrCP- and FBXW7-mediated Mcl-1 degradation, resulting in induction of apoptosis .

BMS-470539 dihydrochloride is a selective and highly potent melanocortin 1 receptor (MC-1 R) agonist with anti-inflammatory activity. BMS-470539 attenuates oxidative stress and neuronal apoptosis via the MC1R/cAMP/PKA/Nurr1 signaling pathway in a neonatal hypoxia-ischemia rat model.

FMP-API-1 is an inhibitor of the A-kinase anchoring protein (AKAP)-PKA interaction. It binds to the allosteric site of the PKAR subunit, enhancing the activity of PKA and AQP2 in PKA knockout cell lines of the renal cortex collecting duct (mpkCCD cells). FMP-API-1 holds potential for studying nephrogenic diabetes insipidus (NDI).

GSK-3α/β-IN-1 is a GSK-3α/β inhibitor with IC50 values of 0.265 μM for GSK-3α and 0.255 μM for GSK-3β. It also inhibits PKA with an IC50 of 0.188 μM. GSK-3α/β-IN-1 effectively reduces cell viability in three glioblastoma (GBM) cell lines (IC50: 3-6 μM over 72 hours) without being toxic to human astrocytes, and it exhibits good metabolic stability. Additionally, it shows potential central nervous system activity in a whole human blood-brain barrier (BBB) GBM model.

Plasma kallikrein-IN-5 (Compound 20) is an effective covalent inhibitor of plasma kallikrein (Pka), with an IC50 of 66 nM at 1 minute and 70 pM at 24 hours. It is used in research related to hereditary angioedema (HAE).

8-CPT-2Me-cAMP sodium is a sodium salt compound that selectively activates exchange proteins activated by cAMP (Epac), which are cAMP-sensitive guanine nucleotide exchange factors (GEFs) responsible for activating small GTPases Rap1 and Rap2. It specifically activates Epac1 with an EC50 value of 2.2 μM, while showing no activation of PKA with an EC50 value greater than 10 μM [1]. Additionally, 8-CPT-2Me-cAMP sodium stimulates the Epac-mediated release of calcium ions (Ca2+) in vitro in pancreatic β-cells [2].

SB-747651A is a potent, ATP-competitive inhibitor of mitogen- and stress-activated kinase 1 (MSK1, IC50 = 11 nM). It targets the N-terminal kinase domain. SB-747651A inhibits MSK1, MSK2, PKA, PKB, RSK and p70S6K activity in cells.

PKC412(Midostaurin (PKC412); CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors.

A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki: 11 nM for Akt1) [1]. It exhibits inhibitory activity against PKA and Cdk2 (IC50: 16 46 nM) but is 10- to >1, 800-fold selective for Akt1 versus additional kinases in th

Paraxanthine (1,7-dimethylxanthine) is a metabolite of caffeine (sc-202514) which functions as an adenosine receptor ligand and a PARP-1 inhibitor in pulmonary epithelial cells. Studies suggest that Paraxanthine is structurally similar to caffeine and possibly mediates the physiological effects of caffeine. Also Paraxanthine acts as a competitive phosphodiesterase inhibitor, which increases intracellular cAMP, activates PKA, inhibits TNF-α and leukotriene synthesis. In addition, Paraxanthine acts as a Na+/K+ ATPase enzymatic effector.

1. Fargesin ((+/-)-Fargesin) as a potential β1AR antagonist through cAMP/PKA pathway could protect against myocardial ischemia/reperfusion injury in rats. 2. Fargesin improves dyslipidemia and hyperglycemia by activating Akt and AMPK in WAT.

Bim-IN-1, a potent inhibitor of Bim expression with low toxicity, effectively reduces Bim expression levels while exhibiting minimal inhibition of protein kinase A (PKA).

1. 8-Gingerol has antioxidant activity. 2. 8-Gingerol has antimycobacterial activity. 3. 8-Gingerol could be used as an effective skin-whitening agent. 4. 8-Gingerol shows antipyretic and anti-inflammation characteristics. 5. 8-Gingerol seems to be effect

1. Nardosinone has inhibitory effect on Ang II-induced hypertrophy in H9c2 cells, might be mediated by targeting PI3K/Akt and MEK/ERK signaling pathways. 2. Nardosinone could protect against the neuronal injury exposed to OGD, which may be relevant to the

PIM1-IN-4 (Compound 8) is a potent inhibitor of PIM1 and also shows significant inhibitory activity against SGK-1, PKA, CaMK-1, GSK3β, and MSK1, making it potentially valuable for cancer research [1].

4′-Demethylnobiletin, a bioactive metabolite, activates the PKA/ERK/CREB signaling pathway, enhances CRE-mediated transcription in hippocampal neurons, and reverses memory impairment linked to NMDA receptor antagonism through ERK signaling stimulation [1].

PKI(5-24) TFA is a synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase) with potent and competitive inhibition properties, exhibiting a K i of 2.3 nM. It corresponds to residues 5-24 of the natural heat-stable protein kinase inhibitor [1][2].

Malantide TFA, a synthetic dodecapeptide, originates from the phosphorylation site targeted by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Exhibiting a high specificity for PKA with a Michaelis constant (Km) of 15 μM, this compound demonstrates more than 90% inhibition of substrate phosphorylation in the presence of protein inhibitor (PKI) across various rat tissue extracts [1]. Moreover, Malantide TFA acts as an effective substrate for Protein Kinase C (PKC) with a Km of 16 μM [2].

Urocortin II, mouse, is a selective and potent endogenous peptide agonist for the type-2 corticotropin-releasing factor (CRF2) receptor, displaying K_i values of 0.66 nM for CRFR2 and >100 nM for CRFR1, signifying its high specificity. It engages CRF2 receptors through mechanisms dependent on cAMP/PKA and Ca2+/CaMKII. Additionally, Urocortin II, mouse is localized in specific regions of the central nervous system, influencing central neurons that process visceral sensory information and regulate autonomic functions [1] [2] [3].

H1-7 (histone H1 phosphorylation site), a synthetic polypeptide, serves as a PKA substrate and demonstrates utility in various PKA substrate applications [1] [2].

PKI (14-24)amide is a potent inhibitor of Protein Kinase A (PKA), effectively inhibiting cyclic AMP-dependent protein kinase activity in cell homogenates [1] [2].