ki app

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.

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].

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

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 inhibitor of aminopeptidase P (APP), with Ki values of 2.6 µM for rat APP and 0.64 µM for human APP. This compound also exhibits cardioprotective properties.

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.

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.