competitive

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.

Flavopiridol hydrochloride (MDL 107826A) is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity.

Punicalagin is a major ellagitannin found in pomegranates that is reported to produce antioxidant, anti-inflammatory, and anticancer effects. It has been shown to prevent high-fat diet-induced obesity-associated accumulation of cardiac triglyceride and ch

Guanidinoethyl sulfonate (Taurocyamine) is a competitive glycine receptor antagonist.

Trimethylammonium chloride is a product of the breakdown of plants and animals and is a non-competitive acetylcholinesterase inhibitor.

Purpurin (Verantin) was a reversible and competitive inhibitor of MAO-A with a Ki value of 0.422μM. it exhibits anti-angiogenic, antifungal, antibiotic, and antioxidative activities.

L-(+)-Arabinose selectively inhibits intestinal sucrase in a non-competitive manner, thereby preventing glucose elevation induced by sucrose intake.

Aminophylline (Phyllocontin) is a competitive nonselective phosphodiesterase inhibitor giving a bronchodilatory effect.

Malonic acid (propanedioic acid) is the archetypal example of a competitive inhibitor: it acts against succinate dehydrogenase (complex II) in the respiratory electron transport chain. Malonic acid is found to be associated with malonyl-CoA decarboxylase deficiency, which is an inborn error of metabolism.

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.

Tolazoline hydrochloride (NSC35110 (hydrochloride)) is a non-selective competitive α-adrenergic receptor antagonist used in treatment of persistent pulmonary hypertension of the newborn.

Decanoic Acid (Caprynic acid) acts as a non-competitive AMPA receptor antagonist.

Dicoumarol (Dicumarol) is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicoumarol is a competitive inhibitor of vitamin K epoxidereductase; thus, it inhibits vitamin K recycling and causes depletion of active vitamin K in blood. This prevents the formation of the active form of prothrombin and several other coagulant enzymes, and inhibits blood clotting.

Sarcosine (Methylglycine) is a competitive inhibitor of the type I glycine transporter (GlyT1) and an N-methyl-D-aspartate receptor (NMDAR) co-agonist.

DL-Norvaline (2-Aminopentanoic acid) is a non-competitive inhibitor of arginase.

Methylmalonic acid is an indicator of vitamin B-12 deficiency in cancer patients.Methylmalonic acid is a competitive succinate dehydrogenase inhibitor.

L-Cysteic acid monohydrate (3-Sulfo-L-alanine Monohydrate) is an oxidation product of L-cysteine that may be used as a competitive inhibitor of the bacterial aspartate: alanine antiporter (AspT) exchange of aspartate and in other aspartate biological systems. L-Cysteic acid monohydrate is used in monomeric surfactant development. L-Cysteic acid monohydrate may be used in studies of excitatory amino acids in the brain, such as those that bind to cysteine sulfinic acid receptors. It is a useful agonist at several rat metabotropic glutamate receptors (mGluRs).

D-Asparagine (H-D-Asn-OH) serves as a nitrogen source for yeast strains and acts as a competitive inhibitor of L-Asparagine hydrolysis with a Ki of 0.24 mM.

Diphylline (Diprophylline) is a xanthine derivative. Diphylline exerts bronchodilator effects and to a lesser extent vasodilator and diuretic properties. Diphylline probably acts as a competitive inhibitor of phosphodiesterase which leads to an increase in intracellular cAMP. This results in relaxation of bronchial smooth muscle and other smooth muscles. Diphylline may also antagonize adenosinereceptors. Diphylline is used in the treatment of acute bronchial asthma, chronic bronchitis and emphysema.

N-Acetylglycine is a minor constituent of food that is not genotoxic or acutely toxic and is capable of being used in biological studies of mimetic peptides.N-Acetylglycine acts as a blocker of the N-terminus of a peptide.3-Hydroxyanthranilic acid is a competitive succinate dehydrogenase inhibitor.

Apigenin (NSC 83244) is an aromatic oil extracted from the flowers or leaves of the daisy-like plants. Extracts, oils and teas made from chamomile are used for its soothing qualities as a sedative, mild analgesic and sleep medication. Apigenin has not been implicated in causing serum enzyme elevations or clinically apparent liver injury.

N4-Benzoyl-2′-deoxycytidine is a synthetic nucleoside analog of the natural nucleoside deoxycytidine (dC), a competitive inhibitor of DNA polymerase. In vitro studies have shown that it inhibits replication in viruses, bacteria and eukaryotic cells. It has also been shown to inhibit tumor cell growth in animal models.

Mesaconic acid (Methylfumaric acid) is used as a fire retardant, as recent studies revealed this acid is a competitive inhibitor of fumarate reduction.

Butyrolactone I (Olomoucin) is an ATP-competitive inhibitor of CDK and cdc2 kinase family. Butyrolactone I shows antitumor effects in non-small cell lung, small cell lung, and prostate cancer cell lines.

Butyl isobutyl phthalate (ButylIsobutylPhthalate) is a non-competitive α-glucosidase inhibitor(IC50 :38 μM),it shows a hypoglycemic effect

Salvianolic Acid C is extracted from the root of Salvia miltiorrhiza, a perennial plant in the genus Salvia.

Chelerythrine Chloride is a cell-permeable inhibitor of protein kinase C, competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.

Bicuculline ((+)-Bicuculline) is a light-sensitive competitive antagonist of GABAA receptors, originally identified in 1932 from plant alkaloid extracts, and isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and various Corydalis species.

Atropine (DL-Hyoscyamine) Sulfate is the sulfate salt of atropine, a naturally-occurring alkaloid isolated from the plant Atropa belladonna. Atropine functions as a sympathetic, competitive antagonist of muscarinic cholinergic receptors, thereby abolishing the effects of parasympathetic stimulation.

α-Conotoxin MII is a highly potent and selective competitive antagonist for α3β2 subunit-containing nicotinic receptors (IC50 = 0.5 - 3.5 nM at α3β2 expressed in Xenopus oocytes). Also potently blocks β3-containing neuronal nicotinic receptors. Displays >

Ajmalicine (Raubasine) (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, IC50 = 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity。

Thiocolchicoside (Thiocolchicine 2-glucoside analog) (Muscoril, Myoril, Neoflax) is a muscle relaxant with anti-inflammatory and analgesic effects. It acts as a competitive GABAA receptor antagonist and also glycine receptor antagonist with similar potency and nicotinic acetylcholine receptors to a much lesser extent. It has powerful convulsant activity and should not be used in seizure-prone individuals.

Ginsenoside F1 (20(S)-Ginsenoside F1) is an enzymatically modified derivative of ginsenoside Rg1, showing competitive inhibition of the activity of CYP3A4 and a weaker inhibition of the activity of CYP2D6.

24-Methylenecycloartanyl ferulate, a compound belonging to the γ-oryzanol family, demonstrates the ability to enhance parvin-beta expression within human breast cancer cells. Furthermore, it exhibits potential as an ATP-competitive Akt1 inhibitor, with an EC 50 value of 33.3 μM.

Thielavin A is a fungal metabolite originally isolated from T. terricola that is related to thielavin B . Thielavin A inhibits COX, blocking both the conversion of arachidonic acid to prostaglandin H2 and the conversion of PGH2 to PGE2 . Thielavin A also inhibits glucose-6-phosphatase in rat liver microsomes (IC50 = 4.6 μM). It is a non-competitive inhibitor of α-glucosidase from S. cerevisiae (IC50 = 23.8 μM; Ki = 27.8 μM).

SL 0101-1 (SL0101) is a selective, efficient, reversible and ATP-competitive inhibitor of p90 ribosomal S6 kinase (RSK) that can permeate cell membranes, with an IC50 value of 89 nM for RSK.SL 0101-1 (SL0101) is also a potent RSK1/2 inhibitor with a Ki value of 1 μM. SL 0101-1 (SL0101) is also a potent RSK1/2 inhibitor with a Ki value of 1 μM.

2-(2,4-Dihydroxyphenyl)-6-hydroxybenzofuran exhibits radical scavenging activities and inhibits mushroom tyrosinase with an IC50 value of 5.2 [micronM], acting as a competitive inhibitor.

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.

Paraxanthine (1,7-dimethylxanthine) is a metabolite of caffeine (sc-202514) which functions as an adenosine receptor ligand and a PARP-1 inhibitor in pulmonary epithelial cells. Studies suggest that Paraxanthine is structurally similar to caffeine and possibly mediates the physiological effects of caffeine. Also Paraxanthine acts as a competitive phosphodiesterase inhibitor, which increases intracellular cAMP, activates PKA, inhibits TNF-α and leukotriene synthesis. In addition, Paraxanthine acts as a Na+ K+ ATPase enzymatic effector.

(-)-Hydroxycitric acid (HCA) can inhibit fat synthesis and reduces food intake, the primary mechanism of action of HCA appears to be related to its ability to act as a competitive inhibitor of the enzyme ATP-citrate lyase, which catalyzes the conversion of citrate and coenzyme A to oxaloacetate and acetyl coenzyme A (acetyl-CoA), primary building blocks of fatty acid and cholesterol synthesis.

4,6-O-Ethylidene-α-D-glucose (Ethylidene-glucose), a derivative of glucose, serves as a competitive inhibitor for the exofacial binding site of glucose transporter 1 (GLUT1), exhibiting a Ki of 12 mM against wild-type 2-deoxy-D-glucose transport.

8-Geranyloxypsoralen inhibits α2-secretase (BACE1) activity in non-competitive manner, with the IC(50) values <25.0 μM, it can induce vasorelaxation on rat arterial tissues. 8-Geranyloxypsoralen possesses nematicidal activities, the median lethal concentrations (LC(50)) is 188.3 mg L against B. xylophilus and is 117.5 mg L against P. redivivus.

Osthenol is a natural product, and is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (Ki=0.26 µM).It shows antitumor-promoting activity, it also has antifungal and antibacterial activities.

Zaragozic acid A trisodium, a metabolite produced by fungi, serves as a reversible competitive inhibitor of squalene synthase.

Tricetin is a flavonoid isolated from pomegranate.Tricetin is a potent competitive inhibitor of Keap1-Nrf2 protein-protein interaction (PPI) and protects Parkinson's disease patients from 6-OHDA-induced neurotoxicity by activating the Nrf2 HO-1 signaling pathway and blocking mitochondria-dependent apoptotic pathways.Tricetin Inhibits migration and expression of the indicator protease progerin-1 (PS-1) in nasopharyngeal carcinoma through the Akt GSK-1β pathway.Tricetin inhibits endothelial inflammation induced by oxidized LDL mediated by Egr-1, and protects rat chondrocytes from IL-1β-induced inflammation and apoptosis.Tricetin is an inhibitor of endothelial inflammation induced by oxidized LDL mediated by Egr-1 and protects against IL-1β-induced inflammation and apoptosis.

N,N',N''-Triacetylchitotriose is a competitive inhibitor of lysozyme.

(±)-Boehmenan shows potent protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity in vitro with the IC(50) values of 43.5 uM, it inhibits PTP1B activity in a competitive manner. Boehmenan exhibits the potent cytotoxic effects against many cancer cell

6-Hydroxykaempferol is a competitive inhibitor of tyrosinase compared to L-DOPA, it shows also high antioxidant activities.