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Description: CK1 inhibitor; displays selectivity for CK1δ and CK1ε
Chemical Name: 1,3-Dihydro-3-[(2,4,6-trimethoxyphenyl)methylene]-2H-indol-2-one
Purity: ≥98% (HPLC)
Biological Activity
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
| M. Wt | 311.33 |
| Formula | C18H17NO4 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 186611-52-9 |
| PubChem ID | 3674 |
| InChI Key | JBJYTZXCZDNOJW-UHFFFAOYSA-N |
| Smiles | COC1=CC(OC)=C(C(OC)=C1)/C=C2C(NC3=C/2C=CC=C3)=O |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 31.13 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 311.33. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.21 mL | 16.06 mL | 32.12 mL |
| 5 mM | 0.64 mL | 3.21 mL | 6.42 mL |
| 10 mM | 0.32 mL | 1.61 mL | 3.21 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.64 mL |
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References
References are publications that support the biological activity of the product.
Behrend et al (2000) 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 5303 PMID: 11103931
Mashhoon et al (2000) Crystal structure of a conformation-selective casein kinase-1 inhibitor. J.Med.Chem. 275 20052 PMID: 10749871
Chia et al (2014) Phosphorylation of LRRK2 by casein kinase 1α regulates trans-Golgi clustering via differential interaction with ARHGEF7. Nat.Commun. 5 5827 PMID: 25500533
If you know of a relevant reference for IC 261, please let us know.
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Keywords: IC 261, IC 261 supplier, IC261, casein, kinase, 1, CK1, inhibitor, inhibits, CK1delta, CK1epsilon, Casein, Kinase, 6676, Tocris Bioscience
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