rp8cptcamps sodium

Rp-8-CPT-cAMP is a structural combination of the lipophilic and non-hydrolyzable cAMP analogs, 8-CPT-cyclic AMP and Rp-cyclic AMPS .[1] It functions as a site-selective inhibitor of protein kinase A (PKA) type I and II, with preference towards site A of type I and site B of type II.2 By occupying cAMP binding sites at the regulatory subunit of PKA, Rp-8-CPT-cAMP prevents the kinase holoenzyme from dissociative activation.[2],[3]

8-Bromo-cGMP sodium is a PKG activator, a membrane-permeable analog of cGMP. 8-Bromo-cGMP sodium has pain-relieving and vasodilatory effects, significantly inhibits Ca2+ macroscopic currents, and inhibits high K+-stimulated insulin release.

D-Fructose-1,6-bisphosphate sodium salt hydrate is the intermediate in carbohydrate metabolism, including glycolysis and gluconeogenesis. During glycolysis, it is produced by phosphorylation of fructose-6-phosphate by phosphofructokinase. The reverse reaction mediated by fructose-1, 6-diphosphatase-1 is one of the rate-limiting steps of gluconeogenesis. The same reaction occurs in the chloroplasts of plants, D-Fructose-1,6-bisphosphate sodium salt hydrate as part of the reducing pentose phosphate cycle. Since cancer cells use glycolysis as a primary source of metabolic energy production, this pathway has become a major target for cancer chemotherapy.

8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt) is a long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinase（PKA）, but resistant to degradation by cyclic AMP phosphodiesterase.

HOIPIN-8 is a potent inhibitor of the linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. As a derivative of HOIPIN-1, it exhibits 255-fold greater inhibition of both petit-LUBAC and TNF-α-mediated NF-κB activation compared to HOIPIN-1. HOIPIN-8 is a promising tool to explore cellular functions of LUBAC.

Rp-Uridine-5'-O-(1-thiotriphosphate) (Rp-UTP-α-S) serves as a nucleotide agonist for purinergic P2Y2 and P2Y4 receptors, effectively inducing inositol phosphate accumulation within 1321N1 astrocytoma cells that express either P2Y2 or P2Y4 receptors, with EC50 values of 5.4 and 27 µM, respectively.

Rp-2'-Deoxyuridine-5'-O-(1-thiotriphosphate) (Rp-dUTP-α-S), a sulfur-containing nucleotide isomer and purinergic P2Y2 receptor agonist, preferentially promotes inositol phosphate accumulation in 1321N1 astrocytoma cells with P2Y2 receptors (EC50 = 12.5 µM) compared to those expressing P2Y4 receptors at a concentration of 10 µM.

8-Chloro-cAMP sodium is a cAMP analog that induces growth arrest and modulates cAMP-dependent PKA activity. This compound also exhibits anticancer activity.

8-Bromo NAD+ serves as a prodrug for the cyclic ADP-ribose (cADPR) inhibitor, 8-bromo cADPR, undergoing conversion to its active form by the enzyme CD38. At a concentration of 1 mM, it effectively inhibits the rise in intracellular calcium levels and chemotaxis triggered by N-formyl-Met-Leu-Phe (fMLP) in mouse bone marrow-derived neutrophils. Furthermore, when applied at 100 µM, this compound reduces LPS-induced nitrite production and decreases the secretion of TNF-α and IL-2 in mouse primary microglial cells.

Rp-8-CPT-cAMPS is a powerful and competitive antagonist of cAMP-induced activation of cAMP-dependent protein kinase (PKA) I and II. Acting as a potent cAMP analog, Rp-8-CPT-cAMPS exhibits a preference for site A of RI over site A of RII. Additionally, it favors site B of RII over site B of RI. This compound effectively inhibits cAMP-dependent PKA activation and demonstrates selectivity in binding to specific sites within the protein kinase.

Rp-Adenosine-5'-O-(1-thiotriphosphate) (Rp-ATP-α-S), a sulfur-containing nucleotide derivative isomer and a purinergic P2Y1 receptor agonist, promotes calcium mobilization in HEK293 cells expressing the human P2Y1 receptor (EC50 = 75 nM). This compound exhibits binding affinity to washed isolated human platelets (Ki = 156 nM) and attenuates ADP-induced aggregation in human platelet-rich plasma (PRP; pA2 = 4.74), as well as inhibits cAMP production triggered by prostaglandin E1 (PGE1) in human PRP (pA2 = 5.26). Furthermore, it triggers relaxation in carbamoylcholine-constricted guinea pig taenia coli strips (EC50 = 56 nM). Rp-ATP-α-S also contributes to the synthesis of cyclic dinucleotides, recognized by bacterial riboswitches.

Rp-8-bromo-Cyclic AMPS (Rp-8-bromo-cAMPS) is a cell-permeable cAMP analog that combines an exocyclic sulfur substitution in the equatorial position of the cyclophosphate ring with a bromine substitution in the adenine base of cAMP. It acts as an antagonist of cAMP-dependent protein kinases (PKAs) and is resistant to hydrolysis by cyclic nucleotide phosphodiesterases. Rp-8-bromo-cAMPS more effectively antagonizes cAMP-dependent activation of purified PKA type I from rabbit muscle than PKA type II from bovine heart.

8-CPT-2Me-cAMP sodium is a sodium salt compound that selectively activates exchange proteins activated by cAMP (Epac), which are cAMP-sensitive guanine nucleotide exchange factors (GEFs) responsible for activating small GTPases Rap1 and Rap2. It specifically activates Epac1 with an EC50 value of 2.2 μM, while showing no activation of PKA with an EC50 value greater than 10 μM [1]. Additionally, 8-CPT-2Me-cAMP sodium stimulates the Epac-mediated release of calcium ions (Ca2+) in vitro in pancreatic β-cells [2].

8-Chloroadenosine-5’-triphosphate (8-chloro ATP), a potent metabolite of the anticancer agent 8-chloro cyclic AMP (cAMP) and a nucleotide derivative, is produced through the biotransformation of 8-chloro cAMP into 8-chloroadenosine, followed by mono- and diphosphate intermediates. Accumulating for up to 12 hours after the administration of 8-chloro cAMP or 8-chloroadenosine, 8-chloro ATP inhibits cell growth, diminishes endogenous ATP levels, and reduces RNA synthesis without affecting DNA synthesis in multiple myeloma cells derived from patients. Moreover, it obstructs topoisomerase II-α-mediated relaxation of supercoiled pUC19 DNA at concentrations ranging from 1.5 to 8 mM and decreases topoisomerase II-α-enhanced ATP hydrolysis by 50% at a concentration of 1 mM in K562 human myelocytic leukemia cells.

cGMP-dependent protein kinase (PKG) inhibitor

Rp-8-Br-cAMPS acts as an inhibitor of PKA. By binding to the cAMP binding sites on the regulatory subunits, Rp-8-Br-cAMPS prevents the dissociation and activation of PKA. Additionally, it enhances immune function in mouse models of retroviral infection.

Cyclic ADP-ribose (cADP-ribose) is a calcium mobilizing nucleotide that is biosynthesized from NAD+ by cADP-ribose synthases, including CD38. cADP-Ribose appears to activate calcium channels in intracellular membranes, which in turn activate ryanodine receptors. 8-bromo-cADP-Ribose is a stable, cell-permeable analog that blocks calcium release evoked by cADP-ribose in sea urchin egg homogenates with an IC50 value of 1.7 μM. It is commonly used to investigate intracellular signaling through cADP-ribose in isolated cells and tissues.

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.

Rp-8-pCPT-cGMPS is a competitive inhibitor of cyclic guanosine monophosphate (cGMP)-dependent protein kinase (PKG) with a Ki of 0.5 μM. This compound exhibits increased lipophilicity, allowing it to penetrate cell membranes more readily and achieve sufficient intracellular concentrations to inhibit PKG. Rp-8-pCPT-cGMPS is useful for researching the activity and function of PKG in platelets.

Rp-Adenosine-5'-O-(1-thiodiphosphate) (Rp-ADP-α-S), a sulfur-containing isomer of the nucleotide derivative ADP-α-S, acts as an inhibitor of phosphorylase kinase with an inhibition constant (Ki) of 0.53 µM. This compound also induces aggregation in isolated human platelets with an effective concentration (EC50) of 20 µM and promotes relaxation in guinea pig taenia coli that has been precontracted with carbamoylcholine, with an EC50 of 58.9 µM.

Rp-Thymidine-5'-O-(1-thiotriphosphate) (Rp-TTP-α-S), an isomer of the sulfur-containing nucleotide derivative TTP-α-S, selectively interacts with HIV-1 reverse transcriptase, exhibiting dissociation constants (Kds) of 45.7, 27.32, and 39.44 µM in the presence of magnesium, manganate, and cobalt, respectively.

8-Bromoguanosine-5'-O-triphosphate, a derivative of guanosine 5'-triphosphate (GTP) - the energy substrate for protein synthesis and gluconeogenesis, acts as an inhibitor of the E. coli GTPase FtsZ with an inhibition constant (Ki) of 31.8 µM. Furthermore, at a concentration of 500 µM, it facilitates the assembly of porcine brain microtubules in a cell-free assay.

8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA) and a potent inhibitor of cyclic GMP-specific phosphodiesterase (PDE VA) with an inhibitory concentration (IC50) of 0.9 μM. It also inhibits PDE III and PDE IV while significantly activating Epac, demonstrating diverse pharmacological activities [1] [2].

Rp-8-Br-cGMPS (Rp-8-bromo-Cyclic GMPS) sodium salt acts as an effective activator of Ca2+-ATPase. Additionally, it serves as an agonist for rod CNG channels and an inhibitor of PKG. Rp-8-Br-cGMPS sodium salt mediates the reduction of cytoplasmic Ca2+ by activating the Ca2+-ATPase enzyme, consequently removing Ca2+ from the cell.

D-fructose-1,6-diphosphate (D-fructose-1,6-diphosphate), also known as Fosfructose, is a cytoprotective natural sugar phosphate. It functions by promoting anaerobic glycolysis, which generates adenosine triphosphate (ATP) under ischemic conditions. This compound holds potential for research in cardiovascular ischemia, sickle cell anemia, and asthma.

Esafosfan trisodium (FDP trisodium) is a cytoprotective natural sugar phosphate for the potential treatment of sickle cell anemia, cardiovascular ischemia and asthma. It acts by stimulating anaerobic glycolysis which generates adenosine triphosphate under ischemic conditions.