T1563

Nifuroxazide (Diarlidan) is an orally available and cell-permeable nitrofuran-based antidiarrheal agent. It has the inhibitory effect against the activation of cellular STAT1/3/5 transcription.

JZP-430 is an effective, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) (IC50: 44 nM). It also shows ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).

Tilmacoxib is a highly selective, time-dependent, and irreversible inhibitor of human COX-2 ( IC50: 85 nM in an enzyme assay).

JTK-853 is a novel, non-nucleoside inhibitor of Hepatitis C Virus (HCV) polymerase, exhibiting effective antiviral activity in HCV replicon cells with EC50s of 0.38 μM for genotype 1a H77 strain and 0.035 μM for genotype 1b Con1 strain.

JW 642 is an effective inhibitor of monoacylglycerol lipase (MAGL) (IC50: 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively).

JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling pathway (IC50: 420 nM).

JYL 1421 (SC 0030) is an antagonist of TRPV1 receptor (IC50 = 8 nM).

K-252a is a protein kinase inhibitor targeting serine-threonine, tyrosine, and CAM kinases. In vitro, it blocks NGF-induced TrkA signalling and neural differentiation, exhibiting antitumour, antibacterial, anti-inflammatory, and neuroprotective activities.

K-252b, an indolocarbazole derived from the actinomycete Nocardiopsis, functions as a protein kinase C (PKC) inhibitor. It is effective in inhibiting extracellular kinases in cultured cells due to its inability to freely cross the cell membrane.

K-252c is a staurosporine analog isolated from Nocardiopsis sp. and is a cell-permeable PKC inhibitor (IC50: 2.45 μM). K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase. K-252c causes apoptosis in human chronic myelogenous leukemia cancer cells.

K-756 is a direct and selective inhibitor of tankyrase (TNKS), inhibiting the ADP-ribosylation activity of TNKS1 [IC50 = 31 nM] and TNKS2 [IC50 = 36 nM].