cyclase

2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor, binding to the P-site with an IC50 of 3 μM.

BIBB 515 is a selective and potent inhibitor of OSC in vivo with an ED50 value of 0.2-0.5 and 0.36-33.3 mg/kg in rats and mice, respectively. 2, 3-Oxidosqualene cyclase (OSC) is an important enzyme in the biosynthesis of animal, plant, and fungal sterols.

Glutaminyl Cyclase Inhibitor 1, a glutaminyl cyclase inhibitor with an IC50 of 0.5 μM, can be utilized for studying neurological disorders.

Glutaminyl Cyclase Inhibitor 3, a designed anti-Alzheimer's compound, is a potent human Glutaminyl Cyclase (GC) inhibitor (IC50: 4.5 nM). It significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions.

Glutaminyl Cyclase Inhibitor 4 is a potent, selective glutaminyl cyclase (QC) inhibitor (IC50: 6.1 nM). It is a potent anti-Alzheimer's agent.

Glutaminyl Cyclase Inhibitor 2 is a glutaminyl cyclase inhibitor with an IC50 of 1.23 μM.

Guanylate cyclase-IN-1 (Example 46) is a specific guanylate cyclase inhibitor used in cardiovascular disease research.

Adenylyl cyclase type 2 agonist-1 is a potent adenylyl cyclase type 2 (AC2) agonist (EC50: 90 nM), and it is a potential lead compound in the fight against respiratory diseases.

Glutaminyl Cyclase Inhibitor 5 is a potent, selective inhibitor of human glutaminyl cyclase (hQC), demonstrating an inhibition concentration half-max (IC 50) of 3.2 nM.

Adenylyl cyclase-IN-1 is a potential adenylyl cyclase inhibitor for ocular hypotonia research [1].

Glutaminyl cyclases-IN-2 (compound 27) serves as a potent inhibitor of glutaminyl cyclase, displaying an IC50 value of 0.08 μM. This compound plays a crucial role in cancer research.

Glutaminyl cyclases-IN-1 (IsoQC-IN-1) is a potent inhibitor of Glutaminyl cyclases (QC), acting on human QC with an IC50 of 12 nM and on isoQC with an IC50 of 73 nM. It selectively inhibits isoQC, blocks CD47 SIRPα interaction, and enhances phagocytosis in THP-1 and U937 macrophages.

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.

Sulfo-ara-F-NMN is an analogue of nicotinamide mononucleotide (NMN) with cellular permeability. Sulfo-ara-F-NMN was selective to activate SARM1 and inhibited CD38 with an IC50 of about 10 μM. Activation by Sulfo-ara-F-NMN to Z-48 or NMN, which has a higher cyclase activity, causes conformational changes in SARM1, resulting in cADPR production, NAD depletion, and non-apoptotic cell death.

NB001 (HTS 09836) is an adenyl cyclase 1 inhibitor that affects both neural and non-neural pain.

Cyclic ADP-ribose (cADPR) is an effective calcium mobilization second messenger synthesized from NAD+ by ADP-ribosyl cyclase. It mainly increases cytosolic calcium through Ryanodine receptor-mediated endoplasmic reticulum release and extracellular influx via the opening of TRPM2 channels.

LY83583 is a soluble guanylate cyclase competitive inhibitor with IC50 of 2 µM.

9-CP-Ade Mesylate (9 CP Ade Mesylate) is a cell-permeable, stable and non-competitive inhibitor of adenylate cyclase.

9-Cyclopentyladenine (NSC-19486) is an adenylate cyclase inhibitor that blocks cellular morphological differentiation and phosphorylation of specific signaling molecules.

Sinitrodil (ITF-296) is a guanylate cyclase stimulant that may be used in the treatment of myocardial ischemia and angina pectoris.

Nicorandil (SG-75)(Ikorel) acts by relaxing the smooth muscle of the blood vessels, especially those of the venous system. It undertakes this through two methods. Firstly, by activating potassium channels, and secondly by donating nitric oxide to activate the enzyme guanylate cyclase. Guanylate cyclase causes activation of cGMP leading to both arterial and venous vasodilatation by de-phosphorylation of the myosin light chain.

Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

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.