PKA Activator

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.

Jaspamycin (Standard) is the analytical standard of Jaspamycin (HY-111759). This product is intended for research and analytical applications. Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC₅₀ of 6.5 nM and K_d of 8 nM in Trypanosoma brucei. Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity.

Methylsilanol acetyltyrosine is an organosilicon derivative that primarily exhibits melanogenesis-promoting, anti-aging, and antioxidant activities. Methylsilanol acetyltyrosine promotes melanin synthesis and distribution by activating the cAMP signaling pathway and enhancing cell communication. Methylsilanol acetyltyrosine can be used in the development of tanning accelerators, as well as photoprotective and anti-photoaging cosmetics.

Sp-6-Phe-cAMPS is a potent, site-selective and membrane-permeable activator of cAMP-dependent protein kinase. Sp-6-Phe-cAMPS does not activate exchange factors directly activated by cAMP and can therefore be used as an Epac negative control. Sp-6-Phe-cAMPS can be used in the study of neurodegenerative diseases.

6-Bn-cAMP is a site-selective activator of cAMP-dependent protein kinase (PKA) which does not activate Epac. 6-Bn-cAMP increases hydrolytic stability against PDE, esterases, amidases and considerably higher membrane permeability compared to cAMP.

Bilobetin (Standard) is the analytical standard of Bilobetin. This product is intended for research and analytical applications. Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.

Pinoresinol dimethyl ether (Standard) is the analytical standard of Pinoresinol dimethyl ether (HY-N2180). This product is intended for research and analytical applications. Pinoresinol dimethyl ether ((+)-Eudesmin) is a non-phenolic furanoid lignin. Pinoresinol dimethyl ether can be isolated from Magnolia biondii. Pinoresinol dimethyl ether activates MAPK, PKC, and PKA upstream pathways and inhibits NO levels. Pinoresinol dimethyl ether has neuroprotective activity.

8-pCPT-5'-AMP is an analogue of 5'-AMP and a lipophilic activator of PKA, PKG and Epac (exchange protein activated by cAMP).

8-PIP-cAMP is a selective cAMP-dependent protein kinase activator and can be used for study of cancer.

8-HA-cAMP is a membrane-permeable cAMP analogue and an activator of cAMP-dependent protein kinase and PKA I. 8-HA-cAMP exerts metabolic stability towards mammalian cyclic nucleotide-responsive phosphodiesterases.

6-Phe-cAMP is a site-selective and highly membrane-permeant activator of protein kinase A (PKA), with a strong preference for site A of both isozymes. 6-Phe-cAMP can undergo phosphorothioate modification.

8-(4-Chlorophenylthio)-cAMP (8CPT-cAMP) is a cell membrane-permeable cAMP analog with excellent membrane permeability, which activates Sgk kinase via phosphorylation mediated by PKA. 8-(4-Chlorophenylthio)-cAMP is hydrolyzed by intracellular enzymes to produce the active metabolite 8CPT-Ade, which induces cortisol synthesis and the expression of steroidogenic protein genes. When used in combination with insulin, 8-(4-Chlorophenylthio)-cAMP enhances the activation of Sgk; it activates the cAMP pathway to promote the proliferation and iodine uptake of thyroid cells. 8-(4-Chlorophenylthio)-cAMP can be used in studies related to metabolism and signal transduction.

6-Bnz-cAMP, a derivative of cyclic adenosine monophosphate (cAMP), is a selective PKA activator with inhibitory activity against the bTREK-1 K⁺ channel. 6-Bnz-cAMP does not activate the Epac signaling pathway. 6-Bnz-cAMP inhibits the bTREK-1 K⁺ channel via a voltage-independent, ATP-dependent mechanism that is independent of the PKA/Epac/calmodulin kinase/MAP kinase pathway. 6-Bnz-cAMP activates CREB phosphorylation to regulate osteoblast-specific gene expression, induces osteoblast differentiation, promotes extracellular matrix mineralization, supports osteoblast proliferation, and shows no cytotoxicity toward osteoblasts. 6-Bnz-cAMP can be used in studies related to bone tissue repair and regeneration.

Bucladesine (Dibutyryl cAMP; DBcAMP) sodium (GMP) is a Bucladesine sodium (HY-B0764) produced by using GMP guidelines. 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.