cAMP is produced by adenylatecyclase (AC), a 12-transmembrane-spanning enzyme that catalyzes the conversion of ATP to 3′,5′-cAMP and pyrophosphate.
In neuronal and neuroendocrine cells, a variety of ligands, such as neurotransmitters and hormones, signal via activation of G protein coupled receptors (GPCRs) coupled to GSα. These receptors activate adenylatecyclases (ACs), the family of enzymes that generate cAMP.
cAMP is synthesized by adenylatecyclases (ACs) and degraded by phosphodiesterases (PDEs). Local cAMP signaling is achieved by targeting of signaling components to subcellular compartments and assembly of signaling complexes. Primary cilia also host several cAMP-signaling components: the somatostatin 3 receptor (SSTR3), various adenylatecyclases (AC3, AC4, AC6, AC8), PKA, and Epac2 (exchange protein directly activated by cAMP).
|Cat. No.||Product Name||CAS No.||Information|
CB-7921220 is a potent, selective Adenylyl Cyclase 1 (AC1) inhibitor.
A potent, selective adenylyl cyclase AC5/6 inhibitor with IC50 of 7.7/17 uM, respectively; displays little to no activity for other AC isoforms (IC50>100 uM); blocks both BAPTA-AM-stimulated cAMP formation and renin release in primary cultures of juxtaglomerular cells.
NB 001 is a potent, relatively selective and orally active adenylyl cyclase 1 (AC1) inhibitor with IC50 of 10 uM (cAMP production inhibition); displays >10-fold selectivity over AC5/6/7/8; shows analgesic effect in animal models of neuropathic pain, without no significant effect on behavioral anxiety.
NKH 477 HCl
NKH 477 hydrochloride (Colforsin dapropate) is a water-soluble analog of Forskolin and a potent activator of adenylyl cyclase, shows some selectivity for cardiac (type V) adenylyl cyclase; increases cAMP accumulation in HEK293 cells stably overexpressing type V more than forskolin; A PKA activator.
A novel potent, specific and allosteric soluble adenylyl cyclase (sAC) inhibitor with IC50 of 3.3 uM in RF-MSS assays; does not inhibit other transmembrane adenylyl cyclases (tmACs) indluding tmACs I, II, V, VIII and IX at 50 uM; binds to the bicarbonate activator binding site and inhibited sAC via a unique allosteric mechanism; inhibits cAMP accumulation in 4-4 cells with an IC50 of 11 uM, and is non-toxic and does not uncouple mitochondria.
A potent, specific soluble adenylyl cyclase (sAC) inhibitor that inhibits Mn2+-dependent sAC with IC50 of 2.7 uM; inhibits physiologically stimulated sAC with similar potency with IC50 of 8.0 uM, completely blocks the capacitation-induced rise in cAMP in wild-type sperm at 10 uM, inhibits in vitro fertilization.
CB-6673567 is a potent, selective Adenylyl Cyclase 1 (AC1) inhibitor with IC50 of 77 uM, displays a 2- to 4-fold isoform selectivity over AC6; blocks the choline-induced cAMP increase in hippocampal neurons.
ST-034307 (ST 034307, ST034307) is a potent, selective adenylyl cyclase 1 (AC1) with IC50 of 2.3 uM; shows no activity against other AC isoforms; inhibits Ca2+-stimulated cAMP accumulation in HEK cells, also inhibits AC1 activity stimulated by forskolin- and Gαs-coupled receptors in HEK-AC1 cells; reduces pain responses in a mouse model of inflammatory pain.
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