adenylyl cyclase (ac)

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.

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).

MANT-GppNHp is a competitive inhibitor of adenylyl cyclase (AC) and a fluorescently labeled GTP analog. It interacts with a hydrophobic pocket near the AC catalytic site through its MANT group, directly obstructing the binding of the substrate ATP. MANT-GppNHp can be utilized in studies of diseases such as cholera, which are associated with increased AC activity.

guanylyl cyclase (GC) and adenylyl cyclase (AC) inhibitor

Mant-GTPγS, an effective GTP analog, displays strong competitive inhibition of adenylyl cyclase (AC). Additionally, it acts as a potent inhibitor of YdeH.

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

2'(3')-O-Anthraniloyladenosine-5'-O-triphosphate (2'-ANT-ATP) and its isomer 3'-ANT-ATP are fluorescent derivatives of ATP that spontaneously isomerize. Emitting a maximum light of 428 nm when excited at 330 nm in water, 2'(3')-ANT-ATP specifically inhibits several types of adenylyl cyclase (AC) including mammalian AC1, AC2, and AC5 with inhibition constants (Kis) of 130, 640, and 120 nM, respectively. It also inhibits Bordetella pertussis AC toxin CyaA with Kis of 1.3 µM (in the presence of manganese) and 20 µM (in the presence of magnesium), Bacillus anthracis AC toxin edema factor with Kis of 0.44 µM (with manganese) and 5.15 µM (with magnesium), and Escherichia coli recombinase A (RecA) with a Ki of 6.3 µM.

TNP-GTP, a fluorescent derivative of guanosine 5'-triphosphate (GTP), essential for protein synthesis and gluconeogenesis, exhibits an emission peak at 552 nm when excited at 410 nm in water. Its fluorescence intensity increases and emission peaks shift to 544 nm and 532 nm in 40% and 80% N,N-dimethylformamide, respectively, due to the solvent's lower polarity compared to water. As a potent inhibitor of glutamate dehydrogenase (Ki = 2.7 μM), TNP-GTP enhances fluorescence and shifts its emission to 545 nm upon binding to this enzyme, a process reversible by GTP addition. Additionally, it serves as an antagonist to purinergic P2X2 and P2X2/3 receptors (IC50s = 0.4 and 1.2 nM, respectively) and selectively inhibits rat soluble guanylyl cyclase (sGC; Ki = 11 nM) over bovine liver glutamate dehydrogenase (GDH; Ki = 2.7 µM) and the calmodulin-dependent B. pertussis adenylyl cyclase (AC) toxin, with inhibition constants of 20 µM and 320 µM in the presence of manganese and magnesium, respectively.

2'(3')-O-Anthraniloylguanosine-5'-O-triphosphate (2'-ANT-GTP) and 3'-ANT-GTP are fluorescent derivatives of GTP that exhibit spontaneous isomerization. 2'(3')-ANT-GTP features an emission peak at 428 nm when excited at 330 nm in aqueous conditions. It functions as an inhibitor of several adenylyl cyclases, notably mammalian adenylyl cyclase 1 (AC1; Ki = 10 nM with manganese), inhibits B. anthracis adenylyl cyclase toxin edema factor (Kis = 4.1 and 13 µM with manganese and magnesium, respectively), and B. pertussis adenylyl cyclase toxin CyaA (Ki = 29 µM with manganese).

MANT-cGMP is a ribose-substituted nucleotide and serves as an adenylyl cyclase (AC) inhibitor with a Ki of 100 μM and a pKi of 4. It is utilized in research focused on heart failure, cancer, and neurological disorders.