Description
NKY-80 (299442-43-6) is a potent and selective adenylyl cyclase inhibitor. Selective for AC5 and over AC3 and AC2 (IC50 = 8.3 μM, 132 μM and 1.7 mM respectively).1,2 More recently shown to indiscriminately inhibit AC6.3 NKY-80 is an extremely useful tool for probing the involvement of adenylyl cyclases in cellular signaling.4
Uses
NKY 80 is an inhibitor of adenylyl cyclase (AC) and displays a greater affinity for AC5 over AC3 and AC2. Adenyl cyclase inhibitors can be easily modified by tumor targeting structures.
General Description
A cell-permeable quinazolinone containing a non-nucleoside compound that acts as a potent, selective inhibitor of adenylyl cyclase (AC) type V isoform (IC50 = 8.3 μM, 132 μM and 1.7 mM for type V, III and II, respectively) in the presence of Gsα GTPγS-Forskolin. Displays ~210-fold greater selectivity for type V over the type II isoform. The inhibition is non-competitive with respect to ATP and Forskolin. Regulates the AC catalytic activity in heart and lung tissues.
Biochem/physiol Actions
Cell permeable: yes
References
1) Onda?et al. (2001),?Type-specific regulation of adenylyl cyclase. Selective pharmacological stimulation and inhibition of adenylyl cyclase isoforms; J. Biol. Chem.,?276?47785
2) Pierre?et al. (2009),?Capturing adenylyl cyclases as potential drug targets; Nat. Rev. Drug Discov.,?8?321
3) Brand?et al. (2013),?Isoform selectivity of adenylyl cyclase inhibitor: characterization of known and novel compounds; J. Pharmacol. Exp. Therap.,?347?265
4) Oritz-Capisano?et al. (2007),?Adenylyl cyclase isoform V mediates renin release from juxtaglomerular cells; Hypertension,?49?618
