Tpl2 Kinase Inhibitor is a reversible naphthyridine ATP-competitive inhibitor of the enzyme Cot (Tpl2 kinase). The enzyme is a hematopoietically expressed serine-threonine kinase responsible for regulating tumor necrosis factor-α, toll-like receptor, and G protein–coupled receptor signaling. Studies suggest that Cot (Tpl2 kinase) inhibitor suppresses LPS-induced (sc-3535) TNF-α production from primary human monocytes. In addition, Tpl2 kinase inhibitor causes an increase in 1,25-Dihydroxyvitamin D3 (1,25D)-induced differentiation of myeloid leukemia cells via inhibition of Cot (Tpl2 kinase).
1. Watford, W.T., et al. 2008. J. Exp. Med. 205: 2803-2812. PMID: 19001140 2. Wang, X., et al. 2010. Cell Cycle. 9: 4542-4551. PMID: 21084834 3. Wang, X., et al. 2010. J. Steroid Biochem. Mol. Biol. 121: 395-398. PMID: 20227498
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KaniarisKaniaris, E. et al. (PubMed 26266915) found that WT mice treated with the Tpl2 Kinase Inhibitor, either prior of after the initiation of high tidal volume ventilation were protected from the development of lung injury, as indicated by preserved lung compliance and lower BALF concentrations of proteins and IL-6, than similarly ventilated, untreated wild-type mice. -SCBT Publication Review
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