Adenylate Cyclase Inhibitor

SQ22536 is an effective adenylate cyclase (AC) inhibitor.

2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor via binding the P-site with an IC₅₀ of 3 µM . 2',5'-Dideoxyadenosine is a nucleoside analog and exerts a potent antiadrenergic action in heart.

SKF-83566 is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a K_i value of approximately 0.4-0.56 nM. SKF-83566 modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway. SKF-83566 acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2). SKF-83566 competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation. SKF-83566 is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect").

cGAS-IN-9 is a cyclic guanosine monophosphate-adenosine monophosphate synthase (cGAS) inhibitor, with IC₅₀ values of 27.5 nM and 5.15 μM against human and murine cGAS, respectively. cGAS-IN-9 shows weak inhibitory activity against human soluble adenylate cyclase, with an IC₅₀ of 26.4 μM. cGAS-IN-9 inhibits dsDNA-induced expression of IFNB1 and CXCL10, as well as activation of the NF-κB pathway, in human immune cells. cGAS-IN-9 can be used in research related to cGAS-dependent inflammatory diseases.

MDL12330A (RMI12330A) is an adenylyl cyclases inhibitor. MDL12330A can inhibit K_V channels, increases insulin secretion and Ca²⁺ levels. MDL12330A accentuates contractions in uterine rings and inhibits cardiac functions. MDL12330A can be used for the research of endocrinology, metabolic and cardiovascular disease .

ST034307 is a potent and selective adenylyl cyclase 1 (AC1) inhibitor, with IC₅₀ of 2.3 μM.

TDI-10229 is a potent and orally bioavailable inhibitor of soluble adenylyl cyclase (sAC, ADCY10). TDI-10229 displays nanomolar inhibition of sAC in both biochemical and cellular assays (IC₅₀ of 195 nM) and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound.

TDI-11861 is an orally active soluble sAC inhibitor optimized and designed based on TDI-10229 (HY-132298), with an IC₅₀ of 3.3 nM and a K_D of 1.4 nM. TDI-11861 has advantages such as high affinity, slow dissociation, and good pharmacokinetics. TDI-11861 can be used for research on male contraception and related sAC pharmacology.

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

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

6-Hydroxyhexanoic acid (6-HHA) is a bacterial effector molecule with metabolic and immunomodulatory activities. 6-Hydroxyhexanoic acid activates the JAK1-STAT1 signaling pathway, promotes phenotypic conversion of M2 macrophages to M1 macrophages, and exerts anti-tumor effects by regulating macrophage polarization. 6-Hydroxyhexanoic acid inhibits lipolysis in adipocytes mediated by Gαi family GPCR, and reduces high-fat diet-induced weight gain and obesity. 6-Hydroxyhexanoic acid can be used in studies related to pancreatic ductal adenocarcinoma, obesity, and insulin resistance.

Zelminemab (AMG-301) is a humanized monoclonal antibody that inhibits PACAP type I (PAC1) receptor.

CCPA (2-Chloro-N6-cyclopentyladenosine) a highly selective A1 adenosine receptors agonist with a K_i of 0.4 nM. CCPA inhibits adenylate cyclase with an IC₅₀ of 33 nM. CCPA exhibits anti-seizure and cardiacprotective activity. CCPA can be used for the research of seizure and myocardial infarction.

Fipexide, a parachloro-phenossiacetic acid derivative, is an orally active nootropic agent. Fipexide reduces striatal adenylate cyclase activity. Fipexide has positive effect on cognitive performance by dopaminergic neurotransmission. Fipexide is used for senile dementia research. Fipexide acts as a chemical inducer in callus formation, shoot regeneration and Agrobacterium infection.

17α,20β-Dihydroxy-4-pregnen-3-one (17,20β-P; 17,20β-DHP) acts as the maturation-inducing hormone (MIH) in salmonid fish and rainbow trout. 17α,20β-Dihydroxy-4-pregnen-3-one binds to oocyte-specific plasma membrane receptors and pertussis toxin-sensitive inhibitory G proteins in fish, inhibits Adenylate Cyclase and reduces intracellular cAMP via the membrane receptor-G protein coupling pathway, thereby initiating downstream signal transduction. 17α,20β-Dihydroxy-4-pregnen-3-one induces de novo synthesis of cyclin B, mediates the translation of cyclin B mRNA and the phosphorylation of cdc2, and promotes the production of maturation-promoting factor (MPF). 17α,20β-Dihydroxy-4-pregnen-3-one drives meiotic maturation of fish oocytes. 17α,20β-Dihydroxy-4-pregnen-3-one is applicable for development-related research.

Fipexide hydrochloride, a parachloro-phenossiacetic acid derivative, is an orally active nootropic agent. Fipexide hydrochloride reduces striatal adenylate cyclase activity. Fipexide hydrochloride has positive effect on cognitive performance by dopaminergic neurotransmission. Fipexide hydrochloride is used for senile dementia research. Fipexide hydrochloride acts as a chemical inducer in callus formation, shoot regeneration and Agrobacterium infection.

NB001 (HTS 09836) is an adenylcyclase 1 (AC1) inhibitor which has effect on neural and non-neural pain by modulating AC1 activity.

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

Guanosine 5'-O-(2-thiodiphosphate) trisodium (GDPβS trisodium) is a non-hydrolyzable derivative of GDP. Guanosine 5'-O-(2-thiodiphosphate) trisodium acts as an inhibitor of adenylyl cyclase (AC) with a K_i value of 600 nM. In the absence of glutamic-pyruvic transaminase (GPT) in cerebral cortex membranes of rodent models, Guanosine 5'-O-(2-thiodiphosphate) trisodium partially activates AC with an EC₅₀ of 400 nM. Guanosine 5'-O-(2-thiodiphosphate) trisodium prevents norepinephrine-induced nitric oxide release in ventricular myocytes.

9-Cyclopentyladenine monomethylsulfonate (9-CP-Ade mesylate) is a stable non-competitive adenylate cyclase inhibitor with cell permeable properties.