Found to have a potent inhibitory action against casein kinase 1 completely with respect to ATP and a much weaker effect on casein kinase 2 and other protein kinases
CKI-7 is a CK1 inhibitor; also inhibits SGK, S6K1 and MSK1. CKI-7 inhibits SGK as potently as CK1. IC50 = 6 μM.
In vivo dose-dependent anti-tumor activity of CKI-7 is demonstrated in a SCID-Beige mouse systemic tumor model utilzing a recently isolated Philadelphia chromosome positive acute lymphoblastic leukemia cell line. Standard cell cycle synchronization studies established that exposure to CKI-7 results in cell cycle dependent caspase 3 activation and apoptotic cell death[2].
CK1: 6 μM (IC50); p70S6K; CK1: 8.5 μM (Ki); Cdc7; SGK; MSK1