NSC139021 (ERGi-USU) is a RIOK2 inhibitor with anticancer activity. RIOK2 can highly selectively inhibit the growth of ERG-positive cancer cells with IC 50 s of 30-400 nM against cell lines. RIOK2 also causes cell cycle arrest and apoptosis in glioblastoma via induction of Skp2 and Skp2-p27/p21-Cyclin E/CDK2-pRb signaling.
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