PKA Activator

Sp-8-CPT-cAMPS, a cAMP analog, is a potent and selective activator of the cAMP-dependent protein kinas A (PKA I and PKA II). Sp-8-CPT-cAMPS selects site A of RI compares to site A of RII by 153-fold and site B of RII compares to site B of RI by 59-fold.

PDE2-IN-1 is a potent and orally active PDE2 inhibitor with an IC₅₀ of 0.6 μM, demonstrating neuroprotective effects. PDE2-IN-1 modulates the PKA/CREB/BDNF signaling pathway by inhibiting PDE2. PDE2-IN-1 improves memory deficits and cognitive impairment in an okadai acid (OKA)-induced Alzheimer’s disease (AD) mouse model. PDE2-IN-1 can be used for the research of AD.

D-Mannitol-d₂ is the deuterium labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β₃-adrenergic receptor (β₃-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells. D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed.

Phosphodiesterase-IN-5 is a potent, orally active and selective phosphodiesterase 10A (PDE10A) inhibitor with an IC₅₀ of 6.2 nM. Phosphodiesterase-IN-5 shows >1612-fold selectivity over other PDEs. Phosphodiesterase-IN-5 exhibits potent antifibrotic efficacy in a Bleomycin (BLM) (HY-108345)-induced murine model of pulmonary fibrosis (PF) by blocking myofibroblast differentiation via the cAMP/PKA/CREB signaling pathway. Phosphodiesterase-IN-5 can be used for the research of PF.

ATP Synthesis-IN-3 (compound 31) is an ATP hydrolysis inhibitor with protective effects during myocardial ischemia. ATP Synthesis-IN-3 can increase the ATP content of ischemic cardiomyocytes, increase the phosphorylation of PKA and phospholamban, and inhibit ischemia-induced apoptosis.

Kiss2 peptide is a positive regulator of reproduction. Kiss2 peptide binds with its cognate receptor Kiss2R (GPR54) in COS-7 cells, activates PKA and PKC signaling pathways through Gas and Gaq proteins, and thus enhances the activity of cAMP response element-dependent luciferase (CRE-luc) and serum response element-dependent luciferase (SRE-luc).

8-CPT-6-Phe-cAMP is an analogue of signal molecule cAMP and a potent protein kinase A (PKA) activator.

Bucladesine (Dibutyryl cAMP; DBcAMP) is a membrane-permeable 3′, 5′-cyclic adenosine monophosphate (cAMP) analog. Bucladesine selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine significantly attenuates MDMA-induced increases in hippocampal mitochondrial ROS formation, mitochondrial outer membrane damage, cytochrome c release, and hippocampal ADP/ATP ratio, thereby improving spatial learning and memory impairments. Bucladesine exhibit anti-nociceptive and anti-inflammation effect. Bucladesine can inhibit cancer cells proliferation, induce apoptosis. Bucladesine can be used for the researches of neurological disease, cancer, inflammation.

Sp-5,6-DCl-cBIMPS is a potent and specific cAMP-dependent protein kinases (cAMP-PK) activator. Sp-5,6-DCl-cBIMPS stimulates insulin release. Sp-5,6-DCl-cBIMPS inhibits U-46619 (HY-108566)-induced activation of Rho, Gq and G12/G13 in platelets.

D-Mannitol-¹³C,d₂ is the deuterium and ¹³C labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β₃-adrenergic receptor (β₃-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells. D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed.

SCR1693 is a selective, reversible, orally active and noncompetitive inhibitor of AChE (IC₅₀ = 0.68 μM) as well as a calcium channel blocker. SCR1693 reduces tau phosphorylation levels, and inhibits the generation and release of Aβ. SCR1693 restores insulin signaling and improves cognitive deficits. SCR1693 can be used for the study of Alzheimer's disease, especially which complicated with type 2 diabetes mellitus.

Sp-5,6-DCl-cBIMPS sodium is a potent and specific cAMP-dependent protein kinases (cAMP-PK) activator. Sp-5,6-DCl-cBIMPS sodium stimulates insulin release. Sp-5,6-DCl-cBIMPS sodium inhibits U-46619 (HY-108566)-induced activation of Rho, Gq and G12/G13 in platelets.

8-Benzylthio-cAMP is a derivative of cyclic adenosine monophosphate (cAMP). 8-Bn-cAMP is a site-selective activator of cAMP-dependent protein kinases. Compared with cyclic adenosine monophosphate, it is more stable to phosphodiesterase (PDE) hydrolysis and has higher membrane permeability. 8-Bn-cAMP can be used to study the role of cAMP in regulating cell proliferation, differentiation and apoptosis.

Linarin (Standard) is the analytical standard of Linarin. This product is intended for research and analytical applications. Linarin (Buddleoside) is an orally active and selective inhibitor of acetylcholinesterase (AChE). Linarin has many activities, such as anti-inflammatory, antioxidant, sleep aid and sedation, bone differentiation, anti-tumor, antibacterial and antiviral. Linarin can be used to study diseases such as the nervous system, osteoporosis and cancer.

D-Mannitol-d is the deuterium labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β₃-adrenergic receptor (β₃-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells. D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed.

Sp-cAMPS (sodium salt) (Standard) is the analytical standard of Sp-cAMPS (sodium salt) (HY-100530C). This product is intended for research and analytical applications. Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM.

8-CPT-cAMP-AM (8-(4-Chlorophenylthio)-cAMP-AM) is an Epac/PKA activator. 8-CPT-cAMP-AM potentiates glucose-dependent first- and second-phase insulin secretion, induces β-cell depolarization, modulates intracellular calcium via influx and ryanodine-sensitive store mobilization, and facilitates calcium-induced calcium release resistant to PKA inhibition. 8-CPT-cAMP-AM can be used for the research of cardiac hypertrophy, diabetic cardiomyopathy, and melanoma.

TC-E 5003 (Standard) is the analytical standard of TC-E 5003 (HY-107574). This product is intended for research and analytical applications. TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC₅₀ of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein K_inase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers.

Sp-cAMPS-AM is an analog of cAMP. Sp-cAMPS-AM acts as the inducer of PKA activation and CREB phosphorylation, through entrance into the cell and release of its parent polar structure Sp-cAMPS.

Sp-8-pCPT-cGMPS is a potent cyclic guanosine monophosphate-gated channel agonist and a lipophilic activator of protein kinase G (types I α, I β, and II) and protein kinase A type II with excellent cell membrane permeability and phosphodiesterase stability. Sp-8-pCPT-cGMPS can be used to study the role of cGMP in neural plasticity and synaptic transmission.