IC261

IC261 is a reversible, ATP-competitive inhibitor of casein kinase 1 (CK1) that inhibits CK1δ and CK1ɛ (IC₅₀ = ~1 µM for both), as well as CK1α (IC₅₀ = 16 µM).¹ It is at least 100-fold less effective against PKA, p34^cdc2, and p55^fyn.¹ IC 261, at 1 µM, inhibits cytokinesis in primary mouse embryo fibroblasts.² IC261 is used to elucidate the role of CK1 in cells and in whole organisms.^3,4,5

WARNING This product is not for human or veterinary use.

1. Mashhoon, N., DeMaggio, A.J., Tereshko, V., et al. Crystal structure of a conformation-selective casein kinase-1 inhibitor. The Journal of Biological Chemisty 275(26), 20052-20060 (2000).

2. Behrend, L., Milne, D.M., Stöter, M., et al. IC261, a specific inhibitor of the protein kinases casein kinase 1-delta and -epsilon, triggers the mitotic checkpoint and induces p53-dependent postmitotic effects. Oncogene 19(47), 5303-5313 (2000).

3. van Ooijen, G., Martin, S.F., Barrios-Llerena, M.E., et al. Functional analysis of the rodent CK1tau mutation in the circadian clock of a marine unicellular alga. BMC Cell Biol. 14, (2013).

4. 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 infection. Antimicrob. Agents Chemother. 58(3), 1501-1515 (2014).

5. Kurihara, T., Sakurai, E., Toyomoto, M., et al. Alleviation of behavioral hypersensitivity in mouse models of inflammatory pain with two structurally different casein kinase 1 (CK1) inhibitors. Mol. Pain 10, (2014).