pac1

PAC-1 (Procaspase activating compound 1) has been used in trials studying the treatment of Lymphoma, Melanoma, Solid Tumors, Breast Cancer, and Thoracic Cancers, among others.

PAC1R antagonist 1 is an orally active PAC1 receptor antagonist that inhibits abnormal pain induced by pituitary adenylate cyclase-activating polypeptide (PACAP) and nerve damage, and may be used in the study of neoplasms and immune-related disorders.

PROTAC BRD4 degrader for PAC-1 (compound 5) is a chimeric BET degrader GNE-987 conjugated with a disulfide-containing linker[1]. This PROTAC-linker conjugate specifically targets and degrades BRD4, enabling selective proteolysis of PAC-1.

Datopotamab deruxtecan (DS-1062) is an antibody-drug conjugate (ADC) that targets tropomyosin 2 (TROP2) on the surface of trophoblast cells. Datopotamab deruxtecan exhibits antitumor activity by specifically binding to TROP2 and internalizing, releasing DXd to inhibit topoisomerase I (IC₅₀ = 0.31 μM), thereby inducing DNA damage and apoptosis. Datopotamab deruxtecan induces significant antibody-dependent cellular cytotoxicity in the presence of peripheral blood lymphocytes and inhibits tumor growth in xenograft models.

Benproperine phosphate (Pirexyl phosphate) is a cough suppressant.

MK 0893 is a potent and selective Glucagon Receptor (GR) antagonist (IC50=6.6 nM) with competitive, reversible, high binding affinity and functional cAMP activity, which attenuates glucagon induced blood glucose elevation and reduces ambient glucose levels in acute and chronic mouse models.

PACAP (1-38), human, ovine, rat (Pituitary Adenylate Cyclase Activating Polypeptide 38), is a neuropeptide comprising 38 amino acid residues.

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

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.

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).

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).

Mahanimbine is found in the roots, leaves and stems of Murraya koenigii and is an orally active alkaloid extracted from Murraya koenigii. Bifidobacterium bifidum leaves on histopathological changes in pancreatic beta cells of streptozotocin-induced diabetic rats.

Asivatrep (PAC14028) is a selective and potent antagonist of transient receptor potential vanilloid subtype 1 (TRPV1) for the study of atopic dermatitis.

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.

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.

MBP Ac1-9, a peptide fragment of myelin basic protein (MBP), serves as an immunodominant epitope in experimental autoimmune encephalomyelitis (EAE) models, where it induces an immune response in T cells leading to pathological changes similar to multiple sclerosis. This peptide is used in research focused on T cell activation and autoimmune responses.

PA-9 is the first small-molecule PAC1 receptor antagonist.

VU0652925 is a PAR4 antagonist. VU0652925 has a P-sel IC50 of 39.2 pM (-pIC50±SEM: 10.41±0.04) and a PAC1 IC50 of 43.0 pM (-pIC50±SEM: 10.4±0.04).

Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.

PA-8 is a small molecule receptor antagonist for PACAP Type I (PAC1) that is selective, effective, and orally active. PA-8 inhibits PacAP-induced CREB phosphorylation at PAC1- receptors, but does not inhibit VPAC1- or vpac2 receptors. PA-8 also inhibited PacAP-induced elevation of cAMP levels in vitro (IC50 = 2 nM) and PacAP-induced aversive response and mechanical atopic pain after intrathecal injection in vivo.

PACAP (1-38) free acid is a deamidated PACAP (1-38) derived from humans, sheep, and rats. PACAP (1-38) free acid can activate the human PAC1 receptor and promote cyclic adenosine monophosphate synthesis in NS‑1 neuroendocrine cells and non-neuroendocrine HEK293 cells.

M65 is a PAC1 receptor-specific antagonist that inhibits the secretion of atrial natriuretic peptide (ANP) [1].

ALD1910 is a humanized monoclonal antibody targeting PACAP38 and PACAP27. It inhibits PACAP signaling through pituitary adenylate cyclase-activating peptide type I receptor (PAC1-R), vasoactive intestinal peptide receptor 1 (VPAC1-R), and VPAC2-R. ALD1910 recognizes a non-linear epitope within PACAP and prevents its binding to cell surfaces. It is useful for studying PACAP-mediated migraines.

PACAP (1-38), human, ovine, rat TFA is an endogenous neuropeptide and a high-affinity agonist for the PAC1 receptor. This 38-amino acid peptide binds to the PAC1 receptor to activate adenylate cyclase, inducing an increase in intracellular cAMP levels and triggering downstream signaling. Research demonstrates that C-terminal amidation of PACAP (1-38), human, ovine, rat TFA is dispensable for its biological activity at the PAC1 receptor, with the non-amidated form retaining full agonistic potency. It plays crucial roles in neuroprotection, regulation of insulin secretion, and vasodilation.