A highly selective dual insulin receptor (IR)/insulin-like growth factor 1 receptor (IGF-1R) inhibitor derived from an extracellular signal-regulated kinase (ERK) inhibitor

Abstract

Background: IR/IGF-1R kinase inhibitors are promising therapeutic agents in cancer. Results: Irfin1, a compound closely related to the ERK inhibitor FR180204, inhibits IR/IGF-1R family kinases. Conclusion: Irfin1 is a remarkably selective inhibitor for the inactive states of IR/IGF-1R kinases. Significance: Broad spectrum kinase inhibitor profiling can be exploited to uncover novel targets of small-molecule compounds. © 2013 by The American Society for Biochemistry and Molecular Biology, Inc.