cAMP

Eriocalyxin B induces apoptosis and cell cycle arrest in pancreatic adenocarcinoma cells through caspase- and p53-dependent pathways, should be considered a candidate for pancreatic cancer treatment; it is a specific inhibitor of STAT3, it directly target

TDI-10229 is a potent and orally available inhibitor of soluble adenylyl cyclase (sAC, ADCY10), displaying nanomolar inhibition of sAC in both biochemical and cellular assays (IC50 = 195 nM). TDI-10229 exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound.

MRE3008F20 is a species-selective and potent adenosine A3 receptor (AA3R) antagonist that inhibits Cl-IB-MECA-induced cAMP production and can be used in glaucoma and asthma studies.13483-88-88-9

CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1; IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively).

UNC0006 is a beta-inhibitory protein biased D(2)R ligand, and is also an antagonist of G(i)-regulated cAMP production and a partial agonist of D(2)R beta-arrestin-2 interaction. It has antipsychotic activity and is used in the study of neurological disorders.

Torbafylline, a xanthine derivative, is a phosphodiesterase (PDE) inhibitor that attenuates burn-induced protein hydrolysis in rat skeletal muscle through activation of the PDE4 cAMP EPAC PI3K Akt pathway, and inhibits the enhanced ubiquitin-proteasome-dependent protein hydrolysis in skeletal muscle of cancer- and sepsis-prone rats.

7-Methoxyrosmanol (7-O-Methylrosmanol) can effectively suppress FSK-induced luciferase expression under the control of the CRE, PEPCK-C and G6Pase gene promoters, it may contribute to its antihyperglycemic activity.

Bithionol (Actamer), formerly marketed as an active ingredient in various topical drug products, was shown to be a potent photosensitizer with the potential to cause serious skin disorders. Approvals of the NDA's for bithionol drug products were withdrawn on October 24, 1967.

ESI-09 is a new-typel noncyclic nucleotide EPAC antagonist.The IC50 values of ESI-09 for EPAC1 and EPAC2 is 3.2 and 1.4 μM, respectively.

Rp-cAMPS sodium is a phosphorothioate analog of cAMP, a protein kinase A inhibitor and a membrane-permeable cAMP antagonist that inhibits cAMP-dependent protein kinases by blocking cAMP-induced conformational transitions, and can be used in the study of cardiovascular diseases.

Atherosperminine shows cholinesterase inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Atherosperminine shows strong anti-plasmodial activity against Plasmodium falciparum, with the IC50 value of 5.80 uM, it also s

ESI-05 (NSC-116966) is a specific EPAC2 (exchange protein directly activated by cAMP 2) antagonist (IC50: 0.4 μM). ESI-05 inhibits cAMP-mediated activation of EPAC2, as well as EAPC2, mediated Rap1 activation.

3-O-Methylquercetin is a selective and competitive PDE3 PDE4 inhibitor, and inhibits PDE3 than PDE4 with a low K(m) value; it inhibits total cAMP- and cGMP-phosphodiesterase (PDE) of guinea pig trachealis at low concentrations.

KH7 is a soluble inhibitor of adenylyl cyclase (sAC)-specific. It has IC50s of 3-10 μM toward both recombinant purified human sACt protein and heterologously expressed sACt in cellular assays. KH7 is also a cAMP inhibitor.

GAT211 (AZ-4) is a selective and potent cannabinoid 1 receptor (CB1R) orthosteric modulator (PAM) with high affinity for cAMP and β-arrestin2.GAT211 has IOP-lowering and antipsychotic effects and can be used in the study of epilepsy.

0990CL is an effective heterotrimer Gαi subunit specific inhibitor, which can interact with purified Go± in GDP-bound state, and can block α2AR mediated cAMP regulation. In the cell model, low concentration of 0990CL could partially restore cAMP level, and high concentration of 0990CL (10μM) began to have negative effects on cell viability.

Adenosine receptor A1 antagonist 5 acts as an adenosine antagonist, is an oxypurine, acts as an insecticide and pest control agent, and has an inhibitory effect on elevated blood pressure.

2-PCCA hydrochloride, a racemate, is a potent and selective GPR88 receptor agonist showing inhibition of GPR88-mediated cAMP production in HEK293 cells with an EC50 value of 116 nM.

EPAC 5376753 is an allosteric inhibitor of EPAC1 with an IC50 of 4 µM in Swiss 3T3 cells.

HJC0350 is an effective and specific EPAC2 inhibitor (IC50: 0.3 μM), and no inhibition of Epac1.

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.

CB1R Allosteric modulator 3 is a potent CB1R modulator that inhibits cAMP and β-Arrestin and can be used for the study of obesity and nicotine addiction.

I942 is a novel, selective ACyclic nucleotide (NCN) EPAC1 agonist that activates exchange proteins to regulate inflammatory gene expression in human umbilical blood tubes and inhibit pro-inflammatory cytokine signaling associated with cardiovascular disease.

ESI-08 is an effective antagonist of EPAC2 with an IC50 of 8.4 μM. ESI-08 selectively blocks cAMP-induced EPAC activation but not cAMP-mediated PKA activation.

GLP-1R modulator L7-028 is a variant that enhances affinity for GLP-1 and (cAMP) signaling.

Citreorosein is a cAMP phosphodiesterase inhibitor, it has anti-inflammatory effect, inhibits proinflammatory cytokines production through the inhibition of both MAPKs and AKT-mediated IκB kinase (IKK) phosphorylation and subsequent inhibition of transcription factor NF-κB activation.

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.

Catalpalactone exhibits high antitermitic, and cytotoxic activities, it exhibits potent inhibitory effects on lipopolysaccharide-induced NO synthesis in RAW 264.7 cells , with IC50 values of 9.80 microM. Catalpalactone can inhibit dopamine biosynthesis by

Fargesone B inhibits the vascular smooth muscle contraction by suppressing the voltage- and receptor-activated calcium influxes in a nonselective manner.

Kushenol A is a kind of Adenosine 3', 5'-cyclic monophosphate(cAMP)phosphodiesterase inhibitiors, it shows selective alpha-glucosidase inhibitory activity. Kushenol A and kushenol C exhibit inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2).

Protopine has antiplatelet effects,which is due to inhibition on thromboxane formation and phosphoinositides breakdown and then lead to the decrease of intracellular calcium concentration.Protopine seems to inhibit the heterotypic cell adhesion between MD

Manassantin A is a high potent HIF-1 inhibitor, it protects the gastric mucosa from ethanol-induced acute gastric injury, and suggest that these protective effects might be associated with COX/PGE2 stimulation, inhibition of iNOS production and NF-κB act

Vulpinic and gyrophoric acids are known as ultraviolet filters for natural lichen populations, they can effectively prevent cytotoxic, apoptotic and cytoskeleton alterative activities of 2.5 J cm(2) UVB in a dose-dependent manner, suggest that vulpinic and gyrophoric acids can be promising cosmetic ingredients to photo-protect human skin cells. Gyrophoric acid also has anti-proliferative cytotoxic effect.

Catalponol can enhance dopamine biosynthesis by inducing TH activity and protect against L-DOPA-induced cytotoxicity in PC12 cells, which was mediated by the increased levels of cyclic AMP.

ent-3-Acetoxy-labda-8(17),13-dien-15-oic acid have vasorelaxant and hypotensive actions, the mechanisms underlying the cardiovascular actions of the labdane involve the activation of the endothelial NO-cGMP pathway, the opening of K+ channels and the alteration on Ca2+ mobilization.

Dodoviscin A may be a new promising pigmentation-altering agent for cosmetic and therapeutic applications, it can inhibit melanin biosynthesis induced by 3-isobutyl-1-methylxanthine and PD98059.Dodoviscin A can promote adipocyte differentiation as charact

Licoarylcoumarin is a strong inhibitor of adenosine 3',5'-cyclic monophosphate (cAMP) phosphodiesterase. Licoarylcoumarin has antibacterial effects on the VRE strains; it has anti-HIV activity, and it has inhibitory effects on xanthine oxidase.

Isopedicin has anti-inflammatory functions, it inhibits the O(2)(*)(-) production in human neutrophils by an elevation of cellular cAMP and activation of PKA through its inhibition of cAMP-specific PDE.

Methyl orsellinate is a phytotoxic compound, it exhibits antifungal activity, it can cause significant inhibition of radicle growth of Amaranthus hypochondriacus and Echinochloa crus-galli, interact with bovine-brain calmodulin and inhibit the activation of the calmodulin-dependent enzyme cAMP phosphodiesterase. Methyl orsellinate can inhibit PTP1B activity with 50% inhibitory concentration values of 277 +/- 8.6 microM, the selective inhibition of PTP1B has been widely recognized as a potential drug target for the treatment of type 2 diabetes and obesity, methyl orsellinate may can treat the type 2 diabetes and obesity.

Trans-caffeic acid stearyl ester is posited to inhibit melanogenesis signaling while suppressing cAMP levels and, subsequently, MC1R, MITF, tyrosinase, TRP-2 and TRP-1 down-regulation, resulting in the suppression of tyrosinase activity, DOPA oxidase activity and melanin synthesis.