Off-White Crystalline Solid
CKI-7 is 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.
ChEBI: A member of the class of isoquinolines that is isoquinoline-8-sulfonamide which is substituted by chlorine at position 5 and in which the sulfonamide nitrogen is substituted by a 2-aminoethyl group. It is an inhibitor of casein kinase I.
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); CK1: 8.5 μM (Ki); Cdc7; SGK; MSK1