ki app

Tyk2-IN-7 is an inhibitor of TYK2 JH2, binds to the TYK2 JH2 domain (IC50: 0.00053 μM; Ki.app: 0.00007 μM).

IQB-782 is a mucolytic agent with mucolytic expectorant activity.IQB-782 inhibits thrombin-activating fibrinolytic inhibitor (TAFI), protects rats from tobacco smoke-induced respiratory obstruction, reduces the viscosity of gastric mucin suspensions in vitro, and may be useful in studies of obstructive lung disease.IQB-782 has been shown to reduce the viscosity of gastric mucin suspensions in vitro.

Ispinesib (SB-715992), a selective, effectvie and reversible inhibitor of kinesin spindle protein (KSP), is derived from quinazolinone, with antineoplastic properties.

GNE-477 is a potent and efficacious dual (PI3K/mTOR) inhibitor.

GDC0084 (RG7666) is a PI3K inhibitor with potential antineoplastic activity. GDC0084 (RG7666) specifically inhibits PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in the inhibition of both cell growth and survival in susceptible tumor cell populations.

CMPD1 is a non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor(apparent Ki (Kiapp): 330 nM).

DI-82 is a highly potent inhibitor of deoxycytidine kinase (dCK), displaying impressive biochemical activity with an IC50 value of 27.8 nM and a K i value of 9.2 nM. Additionally, DI-82 exhibits significant antitumor effects.

Demecarium bromide (BC-48) is a potent cholinesterase inhibitor,and is treatment glaucoma agent.

IMPDH2-IN-2 is a potent inhibitor of inosine 5'-monophosphate dehydrogenase (IMPDH) (Ki,app: 14 μM) and a potential anti-tuberculosis agent, exhibiting moderate antibacterial effects with MIC values of 6.3 and 11 μM in minimal GAST/Fe and rich 7H9/ADC/Tween media, respectively.

FXIIa-IN-1 HCl (Compound 22) is a highly efficient and selective inhibitor of Factor XIIa, with a Ki app value of 97.8 nM, and can be used to study thrombosis and inflammation induced by artificial surfaces.

GNE684 is a potent inhibitor of receptor interacting protein 1 (RIP1) with average Ki app values of 21 nM for human, 189 nM for mouse, and 691 nM for rat RIP1, respectively [1].

Flucopride (Compound 4a) acts as an acetylcholinesterase inhibitor (AChE) with an IC50 value of 24 nM and serves as a partial agonist for the human 5-HT4 receptor (5-HT4R) with a Ki of 9.6 nM for (h)5-HT4R. It promotes non-amyloidogenic processing of APP in COS-7 cells transiently expressing (h)5-HT4R with an EC50 of 23.0 nM. Flucopride is also likely to exhibit significant gastrointestinal tract (GIT) penetration and blood-brain barrier (BBB) permeability, as determined in PAMPA experiments.

Apstatin TFA is a potent, selective aminopeptidase P (APP) inhibitor (Ki=0.64 μM). It exerts cardioprotective effects by increasing local bradykinin levels.

L-685458 (L-685,458) is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM.

Verubecestat (MK-8931) (MK-8931) is an effective and specific β-secretase inhibitor and β-site APP-cleaving enzyme 1 inhibitor or BACE1 protein inhibitor.

LL320 is a selective inhibitor of NNMT, showing a K i,app of 6.8 nM, and interacts with RNMT, DPH5, and SAHH [1].

Apstatin is an effective inhibitor of aminopeptidase P (APP), exhibiting Ki values of 2.6 µM for rat APP and 0.64 µM for human APP. Additionally, Apstatin has cardioprotective properties.