pka

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Gardenin A shows neurotrophic effects via activating MAPK ERK, PKC, and PKA. Gardenin A exhibits antidepressant, anticonvulsant and anxiolytic effects.

Ellagic acid (Gallogen), a thickened tetracyclic natural product, is a potent CK2 inhibitor (IC50=40 nM; Ki=20 nM) with ATP-competitive properties. Ellagic acid is an antioxidant and also possesses antiproliferative activity.

Rottlerin (NSC-56346) is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM). Rottlerin causes apoptosis via caspase 3 activation.

Piceatannol (Astringenin) is an anti-inflammatory, immunomodulatory and antiproliferative agent. It inhibits p56lck and syk protein tyrosine kinases and inhibits NF-κB activation and gene expression of TNF-induced. It is synthetic from the conversion of resveratrol by cytochrome P450 1B1.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

Acefylline (Theophylline-7-acetic acid), a stimulant drug of the xanthine chemical class, acts as an adenosine receptor antagonist. It is combined with diphenhydramine in the pharmaceutical preparation Etanautine to help offset its stimulant effects

Bilobetin ameliorates insulin resistance by PKA-mediated phosphorylation of PPARα in rats fed a high-fat diet.

UCN-02 (7-epi-Hydroxystaurosporine) is a selective and highly potent protein kinase C (PKC) inhibitor produced by Streptomyces N-126 strain, inhibiting PKA. UCN-02 has antitumor activity.

Isopedicin has anti-inflammatory functions, it inhibits the O(2)(*)(-) production in human neutrophils by an elevation of cellular cAMP and activation of PKA through its inhibition of cAMP-specific PDE.

Gliotoxin, a Wnt signaling pathway inhibitor, induces growth inhibition and apoptosis in multiple colorectal cancer cell lines with mutations of the Wnt signaling pathway.

alpha-Amyrin palmitate is antiarthritic in the adjuvant model of arthritis in rats. alpha-Amyrin palmitate is a potent non-competitive inhibitor of chymotrypsin (Ki=6 microM), it also shows weak cytotoxicity against the A2780 human ovarian cancer cell line.

Cycloheterophyllin has an antioxidant effect, it is a photoprotective agent that inhibits ultraviolet A (UVA)-induced oxidative stress and damage, and could be used in the research on and prevention of skin photoaging.

GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SOD (cGMP sodium salt) , also known as cGMP, is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin. GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SOD activates protein kinase G (PKG) and modulates ion channel conductance, with signaling affecting diverse processes including smooth muscle relaxation and proliferation, phototransduction, and energy homeostasis.

Warangalone is an anti-malarial compound that inhibits the growth of Plasmodium falciparum strains 3D7 (chloroquine-sensitive) and K1 (chloroquine-resistant) with IC50 values of 4.8 μg mL and 3.7 μg mL, respectively.

3-Ethoxy-3-oxopropanoic acid (Monoethyl malonic acid) belongs to the class of organic compounds known as dicarboxylic acids and derivatives. These are organic compounds containing exactly two carboxylic acid groups. 3-Ethoxy-3-oxopropanoic acid exists as a solid, soluble (in water), and a weakly acidic compound (based on its pKa). 3-Ethoxy-3-oxopropanoic acid has been primarily detected in blood. Within the cell, monoethyl malonic acid is primarily located in the cytoplasm.

N-Acetylleucine belongs to the class of organic compounds known as leucine and derivatives. Leucine and derivatives are compounds containing leucine or a derivative thereof resulting from reaction of leucine at the amino group or the carboxy group, or fro

N-Acetyl-L-arginine (Ac-Arg-OH), an N-acyl-L-alpha-amino acid with a strong basic nature (based on its pKa), has elevated serum levels in hyperargininemic patients and is associated with several diseases, including uremia and colorectal cancer. In untreated hyperargininemic patients, it reaches its highest levels in cerebrospinal fluid. It has also been detected in apples and loquats, suggesting it could be a potential biomarker for consumption of these foods. Additionally, a low-arginine diet combined with sodium benzoate therapy leads to a marked decrease in plasma N-acetyl-L-arginine concentrations.

3-Methoxyphenylacetic acid belongs to the class of organic compounds known as anisoles. 3-Methoxyphenylacetic acid is slightly soluble (in water) and a weakly acidic compound (based on its pKa).3-Methoxyphenylacetic acid (m-Methoxyphenylacetic acid), a m-hydroxyphenylacetic acid (m-OHPAA) derivative, is a phytotoxin in Rhizoctonia solani. 3-Methoxyphenylacetic acid is used to develop a toxin-mediated bioassay for resistance to rhizoctonia root rot

Histidine (abbreviated as His or H) is an alpha-amino acid. The L-isomer is one of the 22 proteinogenic amino acids, i.e., the building blocks of proteins. It is classified as a charged, polar because of the hydrophilic nature of the imidazole side chain.

Diethyl oxalpropionate (HYL 2-METHYL-3-OXOSUCCINATE), also known as methyloxalacetic acid diethyl ester or diethyl methyloxalacetate, is a member of the class of compounds known as beta-keto acids and derivatives. These compounds are organic compounds containing an aldehyde substituted with a keto group on the C3 carbon atom. Diethyl oxalpropionate is slightly soluble (in water) and a very weakly acidic compound (based on its pKa). Within the cell, diethyl oxalpropionate is primarily located in the cytoplasm.

Calcium 2-hydroxy-4-(methylthio)butanoate (Calcium 2-hydroxy-4-(calcium hydroxymethionine)) is a solid, water-soluble, weakly acidic nutrition enhancer (based on its pKa). This compound, also known as 2-Hydroxy-4-(methylthio)butanoic acid, has been primarily detected in urine and is mainly located in the cytoplasm and adiposome of cells.

1H-Indole-3-carboxaldehyde (3-Formylindole), also known as 3-formylindole or 3-indolealdehyde, belongs to the class of organic compounds known as indoles. Indoles are compounds containing an indole moiety, which consists of pyrrole ring fused to benzene to form 2,3-benzopyrrole. 1H-Indole-3-carboxaldehyde is an extremely weak basic (essentially neutral) compound (based on its pKa). Outside of the human body, 1H-Indole-3-carboxaldehyde has been detected, but not quantified in, several different foods, such as gram beans, brussel sprouts, cucumbers, cereals and cereal products, and white cabbages. This could make 1H-indole-3-carboxaldehyde a potential biomarker for the consumption of these foods. A heteroarenecarbaldehyde that is indole in which the hydrogen at position 3 has been replaced by a formyl group.

Nobiletin (Hexamethoxyflavone) is a natural polymethoxylated flavone isolated from citrus peels with anti-inflammatory and anti-tumor activities. Nobiletin is practically insoluble (in water) and an extremely weak acidic compound (based on its pKa).