Chemical Name: 1,3-Dihydro-3-[(2,4,6-trimethoxyphenyl)methylene]-2H-indol-2-one
Biological ActivityIC 261 is an ATP-competitive casein kinase 1 (CK1) inhibitor. Displays >15 fold selectivity for CK1δ and CK1ε over CK1α (IC50 values are approximately 1 μM for CK1δ and CK1ε and 16 μM for CK1α). Arrests cell cycle at postmitotic G1 phase in cells expressing p53. Inhibits CK1 mediated phosphorylation of LRRK2 in cell lines.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
IC261, a specific inhibitor of the protein kinases casein kinase 1-delta and -epsilon, triggers the mitotic checkpoint and induces p53-dependent postmitotic effects.
Behrend et al.
Crystal structure of a conformation-selective casein kinase-1 inhibitor.
Mashhoon et al.
Phosphorylation of LRRK2 by casein kinase 1α regulates trans-Golgi clustering via differential interaction with ARHGEF7.
Chia et al.
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