camp-signaling

INT-777 (S-EMCA) is a potent TGR5 agonist with an EC50 of 0.82 μM. INT-777 (S-EMCA) inhibits NLRP5-ASC inflammasome-mediated neuroinflammation via the TGR3 cAMP PKA signaling pathway after subarachnoid hemorrhage in rats.

Roflumilast (APTA 2217) is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3', 5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling.

Polygalasaponin F has anti-neuroinflammatory activity, can inhibit the release of inflammatory cytokines TNF-α and NO induced by lipopolysaccharides (LPS) and reduce the expression of inducible nitric oxide synthases. Polygalasaponin F can significantly i

ethyl 1-(4-aminophenyl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate, also known as EAPT, is a potent and selective PDE4 inhibitor that regulates intracellular cyclic adenosine monophosphate (cAMP) levels. It has been used in a variety of scientific applications, including the study of cAMP-mediated signaling pathways, and has potential as a therapeutic agent for the treatment of inflammatory and immune-related diseases.

Panaxydol has anti-cancer activity, can inhibit the growth and apoptosis of cancer cells, the signaling mechanisms involve a [Ca(2+)](i) increase, JNK and p38 MAPK activation, cAMP, MAP kinase and ROS generation through NADPH oxidase and mitochondria.

Luteolin 7-sulfate, derived from the marine plant Phyllospadix iwatensis Makino, suppresses TYR gene expression by intervening in a signaling pathway involving the cAMP-responsive element binding protein (CREB) and microphthalmia-associated transcription factor (MITF). This inhibition ultimately leads to a decrease in melanin synthesis.

2-AHA-cAMP is an analog of the natural signaling molecule cAMP and an activator of cAMP-dependent protein kinase. It features a free terminal primary amine group that can be used for coupling to gels or fluorescent dyes.

CG500354 plays a tumor suppressive role through the cAMP/CREB signaling pathway and is a novel inducer of neural differentiation and growth arrest in primary HUMAN GBM derived cells.

AH 23848 is a Thromboxane antagonist which accelerates inducible nitric oxide synthase degradation through attenuation of cAMP signaling in glomerular mesangial cells.

Abaloparatide (BA 058), a parathyroid hormone receptor 1 (PTHR1) analog and selective activator, promotes Gs cAMP signaling and β-arrestin recruitment, thereby enhancing bone formation and improving cortical structure in mice. This compound holds potential for osteoporosis research [1] [2].

FFA2 allosteric agonist. Inhibits forskolin-induced cAMP increase and stimulates 35SGTPγS binding in biochemical assays (pEC50 values are 6.9 and 7.23, respectively). Binds at allosteric binding site. In functional assays, displays positive allosteric modulation of FFA-induced Gi signaling and negative allosteric modulation of FFA-induced Gq/G11 signaling. Inhibits lipolytic effect of isoproterenol (pEC50 = 5.03) and induces migration of human neutrophils in vitro. Bolognini et al (2016) A novel allosteric activator of free fatty acid 2 receptor displays unique Gi-functional bias. J.Biol.Chem. 291 18915 PMID:27385588 |Sergeev et al (2017) A single extracellular amino acid in free fatty acid receptor 2 defines antagonist species selectivity and G protein selection bias. Sci.Rep. 7 13741 PMID:29061999

AZ7976 (Compound 42), a potent and highly selective agonist for Relaxin Family Peptide Receptor 1 (RXFP1) with a pEC 50 value greater than 10.5, operates through an allosteric mechanism to enhance RXFP1's cAMP signaling, which physiologically elevates heart rate. This property makes AZ7976 a valuable tool in cardiovascular disease research [1].

2'-O-Me-cAMP is an analog of the natural signaling molecule cAMP and serves as a selective activator for the cAMP-activated exchange factor (Epac), characterized by its low membrane permeability.

8-Br-2'-O-Me-cAMP is an analog of the signaling molecule cAMP. It acts as an agonist for cAMP-activated exchange factors (Epac), yet unlike cAMP, it does not activate PKA.

8-CPT-cAMP-AM is a highly membrane-permeable analog of the signaling molecule cAMP. It serves as an activator for both cAMP and cGMP-dependent protein kinases, as well as Epac (exchange protein activated by cAMP).

Serpinin, an agonist of the protease inhibitor Nexin-1 (PN-1), upregulates PN-1 expression via the cAMP-PKA-Sp1 signaling pathway, facilitating granule biogenesis in endocrine cells. It is employed in research on secretory function regulation [1]. Serpinin selectively targets β-adrenergic receptors, particularly interacting with β1-adrenergic receptors to activate the AC-cAMP-PKA pathway, thereby regulating myocardial systolic and diastolic function. Additionally, pGlu-serpinin upregulates Bcl2 mRNA transcription and provides neuroprotective effects [2].

8-pMeOPT-2'-O-Me-cAMP is an analog of the signaling molecule cAMP and serves as an effective stimulator of the cAMP-activated exchange factors (Epac). Unlike cAMP, it does not activate PKA.

15(R)-Prostaglandin D2 functions as a DP(2) receptor (Prostaglandin Receptor) agonist with potential roles in prostatic hormone signaling and exhibits anti-inflammatory properties. It enhances actin polymerization in human eosinophils and elevates cAMP levels in platelets [1].

Skyrin is a fungal metabolite characterized by a bisanthraquinone structure. It interferes with glucagon signaling through adenylate cyclase without binding to the glucagon receptor. At 10 μM, skyrin reduces both glucagon-stimulated cAMP production and glycogenolysis. It does not interfere with epinephrine or glucagon-like peptide 1 effects on these parameters.[1] Reference:[1]. Parker, J.C., McPherson, R.K., Andrews, K.M., et al. Effects of skyrin, a receptor-selective glucagon antagonist, in rat and human hepatocytes. Diabetes 49, 2079-2086 (2012).

HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 is an effective exchange protein. Which straightly activated by cAMP (Epac) antagonist (IC50=5.9 μM for Epac2).

OX04528 is an orally active and potent GPR84 biased agonist.OX04528 inhibits cAMP signaling and may be useful in cancer research.

Cyclic GMP is an endogenous second messenger that initiates interferon production in response to cytoplasmic DNA. It activates the stimulator of interferon genes (STING), triggering a signaling cascade that results in the production of type I interferons and other immune mediators. The conjugate of cyclic GMP and AMP, known as Cyclic-GMP-AMP, can induce the phosphorylation and nuclear translocation of IRF3, thereby enhancing antiviral immune responses. Additionally, Cyclic GMP may activate PDE to degrade cAMP, inhibit the myocardial calcium current ICa, and regulate cardiac contractility. The derivative 8-Br-cGMP exhibits antiplatelet activity, and Cyclic GMP is used in research related to antiviral immunity and cardiovascular diseases.

VIP(6-28)(human, rat, porcine, bovine) is a potent antagonist that counteracts the effects of exogenous vasoactive intestinal peptide (VIP) on cyclic adenosine monophosphate (cAMP) signaling.

Exendin-P5, a selective agonist for GLP-1R, enhances the potency of G protein-mediated signaling through rapid activation of G proteins via transient interactions with the GLP-1R transmembrane domain. This action accelerates cAMP production, pointing to Exendin-P5's potential use in researching metabolic diseases.