adenylyl cyclase

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.

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

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

LRE1 is a specific and allosteric inhibitor of soluble adenylyl cyclase (sAC).

NKY80 regulates the adenylyl cyclase catalytic activity in heart and lung tissues. NKY80 is a non-competitive inhibitor of adenylyl cyclase type V isoform (IC50s: 8.3 µM, 132 µM, and 1.7 mM for type V, III and II, respectively).

ST034307 is an effective and selective inhibitor of adenylyl cyclase 1 (IC50: 2.3 μM).

AC1-IN-1 is a selective inhibitor of adenylyl cyclase type 1 (AC1, IC50 = 0.54 µM).

Wnt pathway inhibitor 3 is a potent AC1 inhibitor (IC50: 45 nM) with antiproliferative activity, suitable for studies to ameliorate osteoarthritis in a mouse model of experimental osteoarthritis.

α-MSH (MSH, amide) is amide stimulates melanocortin 1 receptor that results in the activation of adenylyl cyclase.

Fipexide (Attentil, Vigilor), a psychoactive drug of the piperazine chemical class, was developed in Italy in 1983. It was served as a nootropic drug in France and Italy, mainly for the therapy of senile dementia, but is no longer in common use because of the occurrence of rare drug side-effects including hepatitis and fever.

Lysipressin ([Lys8]-Vasopressin), Induces contraction of the rabbit urinary bladder smooth muscle, activate adenylate-cyclase. Lysipressin is Antidiuretic hormone that have been found in pigs and some marsupial families.

KH7 is a soluble inhibitor of adenylyl cyclase (sAC)-specific. It has IC50s of 3-10 μM toward both recombinant purified human sACt protein and heterologously expressed sACt in cellular assays. KH7 is also a cAMP inhibitor.

SQ22536 (9-(tetrahydrofuran-2-yl)-9h-purin-6-amine) , the adenosine analogue 9-(Tetrahydro-2-furyl)adenine, inhibited adenylate cyclase activity of crude membrane preparations from catfish (Ictalurus melas) and rat isolated hepatocytes in a non-competitive manner.

SKF-83566 is a blood-brain permeable and orally active antagonist of D1-like dopamine receptor and a weaker competitive 5-HT2 receptor antagonist with Ki of 11 nM

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.

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

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.

OS-3-106 is a novel arylamide phenylpiperazines, as partial agonists at the D3R in the adenylyl cyclase inhibition assay.

NKH477 (Colforsin dapropate hydrochloride) is a derivative of forskolin with antidepressant activity. It inhibits ACh-induced Ca2+ mobilization by acting on ionomycin-sensitive storage sites. NKH477 is an adenylyl cyclase activator with bronchodilatory effects, inhibiting the production of CTL, T-cell proliferation in mixed lymphocyte reactions (MLR), as well as IL-2 production and mitogen responses.

AH22921 is an EP4 prostaglandin receptor antagonist with the ability to antagonize the activation of adenylyl cyclase by prostaglandins in CHO cells. It induces a rightward shift in the PGE? concentration-response curve in these cells, functioning as a non-competitive antagonist. AH22921 is selective for the EP4 receptor, inhibiting its activity in CHO cells without affecting the PGE? concentration-response curve in NPE cells that contain the EP2 receptor.

AC10142A, a selective inhibitor of Adenylyl Cyclase Type 1 (Adenylyl Cyclase Type 1), exhibits an IC50 of 0.26 μM. It is utilized in research models of pain.

mAC2-IN-1 (compound 14) is a potent and selective inhibitor of human adenylyl cyclase (mAC) with an IC50 value of 4.45 μM. It exhibits significantly lower activity against mAC1 and mAC5.

Bis-Cl-ANT-ATP (tetrasodium) is a fluorescent ATP derivative that undergoes spontaneous isomerization. It selectively inhibits the adenylate cyclase toxin CyaA of Bordetella pertussis, with greater efficacy than mammalian adenylyl cyclases AC1, AC2, and AC5, exhibiting \[K_i\] values of 16, 1,700, 2,400, and 1,600 nM, respectively. Bis-Cl-ANT-ATP (tetrasodium) can be utilized in pertussis research.

Bis-Br-ANT-ATP(tetrasodium) is a fluorescent derivative of adenosine-5'-triphosphate (ATP). It selectively inhibits the adenylyl cyclase toxin CyaA of Bordetella pertussis with a Ki of 12.6 nM. This compound is utilized in research related to whooping cough.