The Ras/Raf-1 signalling pathway is a well-characterized system that links receptor tyrosine kinase (RTK) activation with changes in gene expression and cell behavior. Raf-1 is a serine/threonine protein kinase that phosphorylates and activates MAPK-kinase (MEK) in response to activation by Ras. ZM 336372 is a...

Raf-1 is a proto-oncogene serine/threonine protein kinase that signals from Ras to the MAPK/ERK signaling pathway. This pathway mediates basic cellular functions, including proliferation, differentiation, and survival. GW 5074 is a potent, selective, and cell-permeable inhibitor of Raf-1 (IC50 = 9 nM). It blocks...

Simvastatin is a competitive inhibitor of HMG-CoA reductase (Ki = 0.12 nM). Simvastatin reduces plasma cholesterol levels in rats and dogs when administered at doses of 1.2 and 8 mg/kg, respectively. Simvastatin suppresses TNF-induced NF-kappaB activation (IC50 = ~13 µM) and potentiates apoptosis in human myeloid...

Fluvastatin is an inhibitor of HMG-CoA reductase (Ki = 0.3 nM for the rat enzyme). It also inhibits the human cytochrome P450 (CYP) isoform CYP2C9 (IC50 = 100 nM). Fluvastatin inhibits oxidized LDL-induced ferroptosis and reverses oxidized LDL-induced decreases in glutathione peroxidase 4 (GPX4) and system Xc-...

Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds that act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor (EGF) receptor kinase block...