ct 1.2

Nitroflurbiprofen (Nitroxybutyl flurbiprofen) is a NO-releasing COX inhibitor and modulates the increased intrahepatic vascular tone in portal hypertensive cirrhotic rats.

CCT129957 is a novel and potent phospholipase C-γ (PLC-γ) inhibitor with an IC50 of about 3 μM and a GC50 of 15 μM.CCT129957 exhibits anticancer activity and inhibits Ca2+ release in squamous cells.

Ponesimod (ACT-128800) is an orally available sphingosine-1-phosphate receptor 1 (S1PR1, S1P1) agonist with potential immunomodulating activity.

VER-49009 (CCT 129397) is a potent Hsp90 inhibitor(IC50 of 25 nM and Kd of 78 nM).

Setipiprant (ACT-129968) is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2, a G protein-coupled receptor for prostaglandin (PGD2), mediates key inflammatory responses related to allergy and asthma. PGD2, produced by mast cells, binds to CRTH2 on blood-borne cells, inducing chemotaxis of Th2 cells, basophils, and eosinophils, and stimulating cytokine release.

CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM, 28-fold greater selectivity for Akt2 than the closely related PKA kinase.

CCT128930 hydrochloride (CCT128930 hydrochloride) is a potent and selective inhibitor of AKT with IC50 of 6 nM. CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50: 168 nM) through the targeting of Met282 of AKT, as well as 20-fold selectivity over p70S6K (IC50: 120 nM).

CCT129202 is an ATP-competitive pan-Aurora inhibitor for Aurora A, Aurora B and Aurora C with IC50 of 0.042 μM, 0.198 μM and 0.227 μM, respectively. It is less potent to FGFR3, GSK3β, PDGFRβ, etc.

CCT129254, an effective Akt inhibitor, reduces the motility of melanoma cells in vivo.