| Description |
CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn[1].
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| Related Catalog |
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| In Vitro |
Used in a competition assay, CNX-500 detects free, uninhibited Btk and is excluded from interaction with Btk previously bonded by CC-292. In Ramos cells exposed to a range of CC-292 concentrations, the amount of Btk captured by the probe is compared with untreated samples and the extent of Btk bonded is demonstrated to be proportional to CC-292 drug concentration[1].
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| References |
[1]. Evans EK, et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J Pharmacol Exp Ther. 2013 Aug;346(2):219-28.
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