A CK1 inhibitor
CKI-7 is an inhibitor of casein kinase 1 (CK1; Ki = 8.5 μM).1 It is selective for CK1 over CK2, PKC, CaM kinase II (CaMKII), and cyclic AMP-dependent protein kinase (IC50s = 90, >1,000, 195, and 550 μM, respectively). CKI-7 inhibits phosphorylation of a peptide substrate by Leishmania CK1.2 by 50% when used at a concentration of 10 μM.2
1.Chijiwa, T., Hagiwara, M., and Hidaka, H.A newly synthesized selective casein kinase I inhibitor, N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide, and affinity purification of casein kinase I from bovine testisJ. Biol. Chem.264(9)4924-4927(1989) 2.Rachidi, N., Taly, J.F., Durieu, E., et al.Pharmacological assessment defines Leishmania donovani casein kinase 1 as a drug target and reveals important functions in parasite viability and intracellular infectionAntimicrob. Agents Chemother.58(3)1501-1515(2014)
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