IndraLab

Statements


8 | 3

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"The strong inhibition of IKKbeta by staurosporine (K (i) = 172 nM) and ADP (K (i) = 136 nM) provides a rationale and structural framework for designing potent ATP-site inhibitors of IKKbeta, which is an attractive drug target for inflammatory diseases."

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"IKK-1 +2 and IKK-2 had similar K (m) values for ATP and GST-biotin-IkappaB (1-54) and were similarly inhibited by staurosporine and two of its analogues K252a and K252b, suggesting that most of the IkappaBalpha kinase activity in the IKK-1 +2 complex may be attributed to IKK-2."

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"Staurosporine can inhibit IKK2 by these regions through the binding of targets and as a reference to other compounds."