IC 261
Chemical Name: 1,3-Dihydro-3-[(2,4,6-trimethoxyphenyl)methylene]-2H-indol-2-one
Purity: ≥98%
Biological Activity
IC 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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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.
Oncogene, 2000;19:5303 -
Crystal structure of a conformation-selective casein kinase-1 inhibitor.
Mashhoon et al.
J.Med.Chem., 2000;275:20052 -
Phosphorylation of LRRK2 by casein kinase 1α regulates trans-Golgi clustering via differential interaction with ARHGEF7.
Chia et al.
Nat.Commun., 2014;5:5827
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