pac-1

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.

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.

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.

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.

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.

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.

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

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.

PROTAC ER Degrader-2 serves as a synthesis intermediate for the production of PAC, a compound that incorporates the ADCs linker and PROTACs, which are subsequently conjugated to an antibody. PAC, exhibits a greater capability to degrade estrogen receptor-alpha (ERα) compared to PROTAC (without the presence of an antibody)[1].

PROTAC ER Degrader-3, an intermediate for the synthesis of PAC, specifically compound LP2. PAC serves as the linker for ADCs and PROTACs that are conjugated to an antibody. Notably, when PAC is conjugated to an antibody, it exhibits enhanced degradation of estrogen receptor-alpha (ERα) compared to PROTAC alone [1].

PAC/NP-IN-1 (Compound 30) is a dual-target influenza inhibitor that specifically binds to nucleoprotein (NP) and the C-terminal domain of the PA protein (PAc). It inhibits the influenza A virus A/WSN/33 (H1N1) with an EC50 of 3.63 μM and an IC50 of 3.08 μM. PAC/NP-IN-1 is utilized in influenza infection research.

PAC-Phe-Val is a potent inhibitor of HIV-1 protease (HIV-1protease) with an IC50 value of 33.10 nM. It forms stable and strong interactions with key active site residues, resulting in high inhibitory efficacy. PAC-Phe-Val is applicable for research in HIV/AIDS.

Cariporide (HOE-642) (HOE-642), an effective NHE1 inhibitor, has inhibitory effects on the degranulation of human platelets, the formation of platelet-leukocyte-aggregates, and the activation of the GPIIb/IIIa receptor (PAC-1).

5'-O-DMT-PAC-dA can be used in the synthesis of oligoribonucleotides[1]. [1]. Schulhof JC, et, al. The final deprotection step in oligonucleotide synthesis is reduced to a mild and rapid ammonia treatment by using labile base-protecting groups. Nucleic Acids Res. 1987 Jan 26;15(2):397-416.

1,3,3,5,5-pentamethylcyclohexan-1-amine hydrochloride, also known as PAC, is a cyclic amine commonly used as a chiral auxiliary in asymmetric syntheses including the Diels-Alder reaction, hydroxyaldol reaction, and Michael addition.

Parameritannin A-1 is a tetrameric proanthocyanidin (PAC) that can be isolated from the bark of plants belonging to the Apocynaceae family. It acts as a COX-2 inhibitor and also suppresses the activity of phospholipase A2 (PLA2).