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It is difficult to overstate the key role played by kinases in regulating cellular activity. By transferring a phosphate from an ATP to a target protein, a kinase can change that protein's ability to interact with other proteins, its subcellular localization or enzymatic activity. Specific inhibition of a kinase can be used to study its role in a particular signal transduction cascade or to elucidate the manner in which it interacts with its substrate. Because many diseases are the result of out-of-control kinases, kinase inhibitors are also a key area of research in drug development. Whether your research focuses on basic science or its application to medicine, you'll want to check out the products listed below. These specific kinase inhibitors will make sure that there is no phosphorylation by the kinase in question.
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InSolutionT Inhibitors: Protein Kinases
Calbiochem
Calbiochem is pleased to offer you several of our popular inhibitors in a convenient, quality tested solution form. Investigating and understanding the mechanism of enzyme inhibition has become the basis of development of pharmaceutical agents. Although activation of enzymes has been exploited therapeutically, most effects are produced by enzyme inhibition that normalizes an overactive pathway. Years of research has shown that inhibitors are useful for mechanistic studies to learn how enzymes interact with their substrates and how to develop drugs that inhibit aberrant biochemical reactions. |
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LY294002 (PI3 Kinase Inhibitor)
Cell Signaling Technology
LY294002 (PI3 Kinase Inhibitor) was shown to act in vivo as a highly selective inhibitor of phosphatidylinositol 3 (PI3) kinase. When used at a concentration of 50 |M, it specifically abolished PI3 kinase activity but did not inhibit other lipid and protein kinases such as PI4 kinase, PKC, MAP kinase or c-Src. LY294002 is soluble in DMSO or ethanol. For use with in vitro or cell-based assays, it may be diluted into aqueous buffers to yield the desired concentrations. For experiments with cultured cells, CST recommends treating the cells with LY294002 for one hour prior to, and for the duration of, the stimulation. |
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SPD304
Sigma-Aldrich
SPD304 is a small molecule inhibitor of TNF-á activity with a novel mechanism of action. It interferes with protein-protein interactions on the contact surfaces of the trimeric TNF-á subunits, displacing one of the trimer units, resulting in dissociation of the trimer and loss of activity at the receptor TNFR1. SPD304 inhibits TNFR1 receptor binding to TNF-á with an IC50 of 22ìM in vitro and inhibits TNF-á-mediated stimulation of IkB degradation in HeLa cells with an IC50 of 4.6 ìM. |
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