Activators & Inhibitors

Orally active protease inhibitor. Known to inhibit trypsin and various inflammatory proteases including plasmin, kallikrein and thrombin.

PD 173074 inhibited the kinase activity of FGFR1 with an IC50 of 25 nM in vitro, while inhibiting Src, the receptors for insulin, epidermal growth factor (EGF) and PDGF, and several serine/threonine kinases with 1000-fold or higher IC50 values. PD 173074 was an ATP-competitive inhibitor of FGFR1, with a Ki of around 40 nM. PD 173074 inhibited autophosphorylation of FGFR1 and VEGFR2 in a dose-dependent manner with IC50s in the range of 1-5 nM and 100-200 nM, respectively.

A-769662 is a potent, reversible activator of AMP-activated protein kinase (AMPK). AMPK is an αβγ heterotrimer and plays an important role in regulating cellular and whole-body metabolism. A-769662 only activates AMPK heterotrimers containing the β1 subunit. A-769662 activates AMPK through the β subunit carbohydrate-binding module and the γ subunit but not the AMP-binding sites. A-769662 stimulated partially purified rat liver AMPK with an EC50 of 0.8 µM and inhibited fatty acid synthesis in primary rat hepatocytes with an IC50 of 3.2 µM.

PP242 is an inhibitor at the kinase domain of the mammalian target of rapamycin (mTOR), which is a Ser/Thr kinase and a cell growth controller. PP242 inhibits mTORC1 more effectively than rapamycin. Unlike rapamycin, PP242 inhibits both mTORC1 and mTORC2 with IC50 values of 0.03 and 0.058 µM, respectively and it can inhibit cap-dependent translation. PP242 functions by blocking the phosphorylation of Akt at S473 and preventing mTOR activation. PP242 exhitibits IC50 values for other kinases of 0.11 µM (JAK2), 0.41 µM (DNAPK), 0.05 µM (PKC?), 0.2 µM (PKCβ I and II), 4.4 µM (EGFR), and1.5 µM (VEGFR2).

Axitinib (AG-013736) is an oral, potent, and selective inhibitor of vascular endothelial growth factor receptors 1 (VEGFR-1), 2 (VEGFR-2), and 3 (VEGFR-3), platelet derived growth factor receptor (PDGFR), and cKIT (CD117).

Forskolin is a cell permeable adenylate cyclase activator which causes an increase in the intracellular concentration of cAMP. This makes it an important hypotensive and vasodilatory agent. Forskolin also affects calcium currents and inhibits PKC (Protein Kinase C)-stimulated MAPK and RAF-1.

Forskolin is a cell permeable adenylate cyclase activator which causes an increase in the intracellular concentration of cAMP. This makes it an important hypotensive and vasodilatory agent. Forskolin also affects calcium currents and inhibits PKC (Protein Kinase C)-stimulated MAPK and RAF-1.

XAV 939 is a small molecule and selective Wnt pathway transcription factor - catenin-mediated transcription inhibitor and axin stabilizing agent. It stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex and stabilizes axin by inhibiting the poly-ADP-ribosylating enzymes tankyrase 1 (TNKS1) and tankyrase 2 (TNKS2).

ABT-888 (Veliparib) is a potent inhibitor of both PARP-1 and PARP-2. In the MX-1 breast xenograft model (BRCA1 deletion and BRCA2 mutation), ABT-888 potentiated cisplatin, carboplatin, and cyclophosphamide, causing regression of established tumors, whereas with comparable doses of cytotoxic agents alone, only modest tumor inhibition was exhibited.