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Soluble in DMSO. Merck 5, also known as Pyridone 6, is a potent and reversible ATP-competitive inhibitor of the JAK kinases (JAK1, JAK2, JAK3, and Tyk2) with IC(50) values in the low anomolar range. At higher values (IC(50) >100nM) Merck 5 also can inhibit ERK kinase family and appear to block IL-2 and IL-4 dependent proliferation of CTLL cells and inhibits the phosphorylation of STAT5. In research comparing Merck 5 (Pyridone 6) to the Jak inhibitor AG490, Merck 5 demonstrated much lower effective drug concentrations and faster kinetics and appear to be a more sensitive and specific inhibitor of JAK-STAT3 activity compared with AG490 and potently inhibited the growth of primary myeloma cells and myeloma-derived cell lines grown on bone marrow-derived stromal cells . Target: JAK , Kinase Group: PTK , Substrate: Tyrosine
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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