camp-signaling

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).

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.

Trans-caffeic acid (3,4-Dihydroxybenzeneacrylic acid) can be used as a highly sensitive fluorescent probe for the detection of laccase in food and can also stimulate the growth of germ tissue.

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.

Setmelanotide (RM-493) is a selective melanocortin-4 receptor agonist with EC50 values of 0.27 and 0.28 nM for human and rat MC4R. Setmelanotide enhances cAMP signaling, demonstrates functional selectivity, activates sympathetic preganglionic neurons to influence blood pressure, and is widely used to probe MC4R-MRAP2 interactions. Setmelanotide contributes to obesity-related research by modulating hunger and satiety circuits, reversing risperidone-induced weight gain in mice, and helping characterize MC4R variants in pediatric metabolic disorders. The anti-inflammatory actions of Setmelanotide in astrocytoma cells and the utility in combination with calorie restriction further highlight its broad value in metabolic and neuroendocrine research.

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.

PDE1-IN-8 (Compound 3f) acts as an inhibitor of PDE1, with an IC50 of 11 nM. It hinders cAMP and cGMP signaling pathways, impeding the differentiation and proliferation of cells into myofibroblasts, and demonstrates antifibrotic effects in the Bleomycin-induced rat model of pulmonary fibrosis.

Mtb-IN-10 (Compound P15) is an Rv1625c/Cya activator that influences the growth of Mycobacterium tuberculosis (Mtb) by modulating cAMP metabolism. It demonstrates an anti-tuberculosis activity with an EC50 of 1.96 µM in Mtb-infected macrophage models and achieves an oral bioavailability of 58.0% when administered orally to mice at 20 mg/kg. Mtb-IN-10 potentially regulates intracellular signaling and disrupts cholesterol metabolism within Mtb, thereby inhibiting bacterial proliferation. It holds promise for tuberculosis (TB) research, particularly targeting multidrug-resistant (MDR-TB) and extensively drug-resistant (XDR-TB) strains of Mtb.

LNS8801 is an orally active agonist of the G protein-coupled estrogen receptor (GPER). By activating GPER, LNS8801 mediates downstream signaling pathways, such as promoting cAMP production and activating CREB signaling, which results in antitumor activities like inhibiting tumor cell proliferation, inducing cell differentiation, and enhancing tumor immunogenicity. It is applicable in research across various cancers, such as melanoma, pancreatic cancer, colorectal cancer, and lung cancer, as well as studies exploring the role of GPER in normal physiological and pathological processes.

PDE4-IN-1 is a PDE4 inhibitor characterized by high potency (IC50: 8.6 nM) and superior selectivity over other PDE subtypes. This compound inhibits the release of inflammatory cytokines and chemokines. Additionally, PDE4-IN-1 significantly restores the damaged cAMP-CREB signaling pathway, inhibits proliferation, and promotes differentiation to reverse psoriasis formation.

PDE10A-IN-5 (Compound A30) is an orally active inhibitor of phosphodiesterase 10A (PDE10A) with an IC50 value of 3.5 nM. By inhibiting PDE10A, it activates the cyclic adenosine monophosphate (cAMP)-related signaling pathway, exhibiting activity against pulmonary vascular remodeling. This compound is applicable to research in the field of pulmonary arterial hypertension.

6-Bnz-cAMP (N6-Benzoyl-cAMP) is a derivative of cyclic adenosine monophosphate (cAMP) known as an effective inhibitor of the bTREK-1 potassium channel. It strongly suppresses the bTREK-1 potassium channel through a mechanism independent of protein kinase A (PKA). Additionally, 6-Bnz-cAMP can be utilized to investigate potential signaling proteins within the cAMP signaling pathway.

OX04529 (compound 69) is a potent and orally active GPR84 selective agonist. It inhibits FSK-induced cAMP production with an EC50 of 0.0185 nM and demonstrates exceptional potency along with significant bias towards G protein signaling pathways.

A2AR modulator-1 (Compound 45) is a selective negative allosteric modulator of the adenosine A2a receptor (A2aR), with an IC50 value of 9 nM. It reduces the affinity of endogenous adenosine for the receptor and inhibits the activation of the cAMP signaling pathway. A2AR modulator-1 effectively restores pCREB phosphorylation in CD4+ T cells, reverses immunosuppression in the tumor microenvironment, and shows potential in inhibiting tumor growth and metastasis in a triple-negative breast cancer model.

GLP-1R modulator-1 (Compound 384) is a potent and orally active selective agonist of the glucagon-like peptide-1 receptor (GLP-1R). It activates G protein-coupled signaling, leading to increased intracellular cAMP levels, enhanced insulin secretion, delayed gastric emptying, and reduced appetite. GLP-1R modulator-1 holds potential for research in type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).

5-Benzyloxytryptamine (5-BT) is a selective partial agonist of the 5-hydroxytryptamine 1D/1B (5-HT1D/1B) receptors, with an IC50 value of 40 nM for the bovine caudate nucleus 5-HT1D. It exhibits much lower affinity for other receptors (5-HT2 IC50 > 470 nM). 5-Benzyloxytryptamine inhibits adenylate cyclase, leading to reduced neurotransmitter release and downregulation of cAMP signaling. It holds potential for research into diseases associated with neurotransmitter imbalances.

ST171 is a dual-action 5-HT1AR agonist with a Ki of 0.41 nM. It selectively activates the Gi/o signaling pathway and inhibits cAMP accumulation mediated by 5-HT1AR, without Gs activation and with minimal β-arrestin recruitment. ST171 reduces hypersensitivity in mouse models of chronic neuropathic and inflammatory pain and is applicable for pain research.

D1/D5 Receptor agonist-1 is an orally active D1/D5 receptor agonist with the ability to cross the blood-brain barrier. It demonstrates significant efficacy in the cAMP pathway and β-arrestin recruitment, with EC50 values of 3.7 nM for D1R cAMP, 91 nM for D1R β-arrestin, and 129 nM for D1R internalization, and a Ki value of 111 nM for D1R binding affinity. In rats, D1/D5 Receptor agonist-1 inhibits β-arrestin signaling involved in L-DOPA-induced dyskinesia. This compound is applicable in Parkinson's disease research.

6-Bnz-cAMP is a PKA-selective activator. It regulates the PKA dependent signaling pathways. The proliferative signaling pathway which activated by the 6-Bnz-cAMP involves activation of the epidermal growth factor receptor and ERK1/2. Extending the duratio

SW106 is a selective antagonist of PTHR1-mediated cAMP signaling, not functioning as an inverse agonist on either PTHR1-T410P or PTHR1-H223R, which have activating mutations at the cytoplasmic ends of TMD helices-2 and -6, respectively.

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.

Skyrin is a natural bis-anthraquinone derivative and receptor-selective glucagon antagonist that inhibits the growth of HeLa, Vero, K562, Raji, Wish, and Calu-1 tumour cell lines.

ZQ-16 is a potent and highly selective agonist for the G protein-coupled receptor GPR84, demonstrating a half-maximal effective concentration (EC50) of 0.213 μM, and it activates multiple downstream signaling pathways including calcium mobilization, inhibition of cAMP accumulation, phosphorylation of extracellular signal-regulated protein kinase 1/2 (ERK1/2), receptor desensitization and internalization, and receptor-β-arrestin interaction, making it a useful tool compound for studying GPR84 function and a candidate for further optimization.