non-competitive

GW4869 (GW69A) is a selective and non-competitive inhibitor of neutral sphingomyelinase N-SMase (IC50=1 μM). GW4869 also inhibits exosome synthesis/release and is commonly used in exosome-related studies.

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.

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

ART558 is a potent, selective, low molecular weight, allosteric DNA polymerase activity of Polθ inhibitor (IC50=7.9 nM). ART558 can be used for the research of cancer.

Sulindac sulfide (cis-Sulindac sulfide) is a non-steroidal anti-inflammatory compound that has a high affinity for COX-1 and acts as an inhibitor in Ras activation of Raf-1. Sulindac sulfide is a non-competitive inhibitor of gamma-secretase with an IC50 value of 20.2 μM. It is an active metabolite of sulinic acid.

L-(+)-Arabinose selectively inhibits intestinal sucrase activity in a non-competitive manner, inhibiting glucose elevation caused by sucrose intake.

L-Hyoscyamine sulfate (Levsin Sulfate) is the sulfate salt of a belladonna alkaloid derivative and the levorotatory form of racemic atropine isolated from the plants Hyoscyamus niger or Atropa belladonna, which exhibits anticholinergic activity. Hyoscyamine functions as a non-selective, competitive antagonist of muscarinic receptors, thereby inhibiting the parasympathetic activities of acetylcholine on the salivary, bronchial, and sweat glands, as well as the eye, heart, bladder, and gastrointestinal tract. These inhibitory effects cause a decrease in saliva, bronchial mucus, gastric juices, and sweat. Furthermore, its inhibitory action on smooth muscle prevents bladder contraction and decreases gastrointestinal motility.

Tolazoline (Benzalolin), a non-selective competitive α-adrenergic receptor antagonist, is used as a vasodilator to treat spasms of peripheral blood vessels. It has also been used successfully as an antidote to reverse the severe peripheral vasoconstriction as a result of overdose with certain 5-HT2A agonist drugs.

DNQX disodium salt is a water-soluble form of selective antagonist of non-NMDA receptor

Darbufelone (CI-1004) is a non-competitive dual inhibitor of PGF2α and LTB4. Dabfilon effectively inhibits PGHS-2 with a Ki of 10 μM and IC50s of 0.19 μM and 20 μM for PGHS-2 and PGHS-1.

[Ala107]-MBP (104-118) acetate ([Ala107]-MBP ) is synthetic peptide analog of bovine myelin basic protein (MBP). Non-competitive inhibitor of PKC (IC50 = 46 - 145 mM).

N20C hydrochloride (2-((3,3-diphenylpropyl)amino)acetamide hydrochloride) is a non-competitive NMDA receptor open-channel blocker.

SP-146 is a selective, potent and non-ATP-competitive Aurora B inhibitor(IC50 : 0.316 nM).

CK2α-IN-1 is a selective non-ATP-competitive CK2α inhibitor with an IC50 of 7.0 µM and a Ki of 1.6 µM.CK2α-IN-1 exhibits potential anticancer activity and can be used in cancer research.

MB-07729 is a potent non-competitive inhibitor of fructose-1,6-bisphosphate with IC50 values of 189, 121 and 31 nM in rat, monkey and human, respectively, for the study of diabetes.

Ac-Phe-NH2 is a non-competitive inhibitor of polyubiquitin chain elongation at Ki value of 8 ± 1.2 mM.

Laniquidar TFA (R101933) is a novel orally available non-competitive P-glycoprotein (P-gp) inhibitor with an IC50 value of 0.51 μM.Laniquidar has limited bioavailability and can be used to modulate the multidrug resistance transporter.Laniquidar can be used for the study of AML and myelodysplastic syndrome (MDS). Laniquidar is used to study acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS).

Monatepil maleate (AJ-2615 maleate) is an orally active Ca2+-channel and α1-adrenoceptor antagonist and non-competitive heparanoyl-coenzyme A:cholesterol acyltransferase (ACAT) inhibitor with antihypertensive activity.Monatepil maleate is used in studies of hyperlipidemia and atherosclerosis. Monatepil maleate is used to study hyperlipidemia and atherosclerosis.

Catestatin acetate is a non-competitive antagonist of nAChR and inhibits catecholamine release. Catestatin acetate regulates cardiac function and blood pressure.

Aptiganel (CNS-1102) is a non-competitive NMDA antagonist, a peptide that may be used to study acute ischemic stroke.

Tuna AI acetate is an inhibitor of angiotensin-converting enzyme (ACE) in non-competitive manner derived from tuna muscle.

LXE408 fumarate is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 fumarate has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 fumarate has a low propensity to cross the blood brain barrier. LXE408 fumarate has the potential for visceral leishmaniasis (VL) research.

Alaproclate is a non-competitive NMDA receptor antagonist and a new selective 5-HT uptake inhibitor for the study of depression and dementia.

Crilvastatin (PMD 387) is a novel non-competitive hydroxymethylglutaryl coenzyme A reductase inhibitor with cholesterol-lowering activity that inhibits cholesterol uptake in rats with hereditary hypercholesterolemia.

Epristeride (ONO-9302) is an orally active, selective and non-competitive steroidal 5-α-reductase isoform 2 inhibitor that inhibits SR isoform 2.Episteride reduces prostate size and improves symptoms in men with BPH.Episteride induces atrophy and apoptosis of the ventral prostate in rats.

CFM-2, a potent and selective non-competitive antagonist of AMPAR (AMPAR), exhibits anticonvulsant activity across various seizure models.

Laniquidar (R101933) is a third generation non-competitive inhibitor of P-glycoprotein (P-gp) (IC50: 0.51 μM) with limited oral bioavailability. It can also be used to modulate multidrug resistance transporters.

P053 is a potent, non-competitive and selective ceramide synthase 1 (CerS1) inhibitor with an IC50 of 0.5 μM. P053 is an endogenous inhibitor of mitochondrial fatty acid oxidation in muscle and regulator of whole-body adiposity[1].

Fluspirilene (R 6218) is a non-competitive L-type calcium channel antagonist (IC50: 0.03 μM).Fluspirilene is a long-acting antipsychotic compound used in the treatment of schizophrenia.

BPDBA is an effective, selective, and non-competitive inhibitor of the betaine GABA transporter (BGT-1), displaying inhibitory activity against human BGT-1 and mouse GAT2, with IC50 values of 20 μM and 35 μM, respectively.

BMS-593214 is a selective active site-directed factor VIIa inhibitor and a non-competitive inhibitor of the VIIa-activated substrate, FX, with antithrombotic and antihemorrhagic activity.BMS-593214 can be used to study electrically-induced carotid artery thrombosis (AT) and wire-induced vena cava thrombosis (VT).BMS-593214 has been shown to be an antithrombotic inhibitor of the VIIa activating substrate, FX, with antithrombotic and antihemorrhagic activity.

Refametinib (RDEA119) (RDEA119, Bay 86-9766) is an effective, ATP non-competitive and specific inhibitor of MEK1/2 (IC50: 19/47 nM).

DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase σ (PTPσ) inhibitor with IC50 of 1.43 μM. DJ001 promotes the regeneration of hematopoietic stem cells.

MK-8033 hydrochloride is an effective and orally active dual inhibitor of ATP competitive c-Met/Ron, with 1 nM for c-Met and 7nM for Ron IC50. MK-8033 hydrochloride has a high affinity for activated kinase conformation, and is suitable for the study of breast cancer, bladder cancer, and non-small cell lung cancer (NSCLC).

9-CP-Ade Mesylate (9 CP Ade Mesylate) is a cell-permeable, stable and non-competitive inhibitor of adenylate cyclase.

ML141 (CID-2950007) is an effective, specific and reversible non-competitive inhibitor of Rho family GTPase cdc42 (IC50: 200 nM).

U0126, an effective and selective non-competitive inhibitor of MAP kinase, inhibits MEK-1 and MEK-2 with IC50 values of 0.07 and 0.06 μM respectively. U0126 inhibits autophagy and mitophagy.

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.

U0126-EtOH (U0126 Ethanol) is a non-ATP competitive specific inhibitor of MEK1 2 (IC50: 0.07 0.06 μM).

Tideglusib (NP031112), a non-ATP competitive inhibitor of glycogen synthase kinase 3 (GSK-3), is with anti-inflammatory and neuroprotective activities.

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

Mirdametinib (PD325901) is an MEK inhibitor (IC50=0.33 nM) with selective, non-ATP-competitive, and oral activity. Mirdametinib exhibits antitumor activity by inhibiting p-ERK1 2 expression and inducing apoptosis.

PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.

Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.

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.

CI-1040 (PD 184352) (PD184352) is an ATP non-competitive MEK1 2 inhibitor (IC50: 17 nM).

Ned 19 is a selective membrane-permeant non competitive antagonist of NAADP and strongly inhibits tumor growth and vascularization as well as lung metastases in mice.

Astemizole (Laridal) is a synthetic piperidinyl-benzimidazol derivative with antiallergic properties, acts as a reversible competitive inhibitor of histamine H1 receptors, with less anticholinergic effects compared to related agents. It is a long-acting, non-sedative antihistaminic used in the treatment of seasonal allergic rhinitis, asthma, allergic conjunctivitis, and chronic idiopathic urticaria.

Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.

AZD8330 (ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.

L-Phenylalanine (3-Phenyl-L-alanine) is an essential amino acid and the precursor of the amino acid tyrosine, acts as an antagonist at α2δ calcium channels.

D-Phenylalanine, a necessary aromatic amino acid, is a precursor of thyroxine, dopamine, melanin, and noradrenaline (norepinephrine).