For research use only. Not for therapeutic Use.
IC261（Cat No.:I002409）is a potent inhibitor of casein kinase 1 (CK1), an enzyme involved in regulating various cellular processes such as circadian rhythms, cell division, and Wnt signaling. By inhibiting CK1, IC261 disrupts critical signaling pathways, leading to effects on cell cycle progression and apoptosis, making it valuable for cancer research. It is commonly used in studies exploring CK1’s role in tumorigenesis, cellular stress responses, and neurodegenerative diseases. IC261’s ability to target CK1-dependent pathways provides insight into potential therapeutic strategies for cancers and other diseases involving abnormal CK1 activity.
| Catalog Number | I002409 |
| CAS Number | 186611-52-9 |
| Synonyms | (E)-3-(2,4,6-trimethoxybenzylidene)indolin-2-one |
| Molecular Formula | C₁₈H₁₇NO₄ |
| Purity | ≥95% |
| Target | CK1 |
| Solubility | DMSO: ≥ 33 mg/mL |
| Storage | Store at -20°C |
| IC50 | 16 μM |
| IUPAC Name | (3E)-3-[(2,4,6-trimethoxyphenyl)methylidene]-1H-indol-2-one |
| InChI | InChI=1S/C18H17NO4/c1-21-11-8-16(22-2)14(17(9-11)23-3)10-13-12-6-4-5-7-15(12)19-18(13)20/h4-10H,1-3H3,(H,19,20)/b13-10+ |
| InChIKey | JBJYTZXCZDNOJW-JLHYYAGUSA-N |
| SMILES | COC1=CC(=C(C(=C1)OC)/C=C/2\C3=CC=CC=C3NC2=O)OC |
| Reference | </br>1:State-dependent block of voltage-gated sodium channels by the casein-kinase 1 inhibitor IC261. Föhr KJ, Knippschild U, Herkommer A, Fauler M, Peifer C, Georgieff M, Adolph O.Invest New Drugs. 2017 Jun;35(3):277-289. doi: 10.1007/s10637-017-0429-0. Epub 2017 Feb 6. PMID: 28164251 </br>2:Microtubules depolymerization caused by the CK1 inhibitor IC261 may be not mediated by CK1 blockage. Stöter M, Krüger M, Banting G, Henne-Bruns D, Knippschild U.PLoS One. 2014 Jun 17;9(6):e100090. doi: 10.1371/journal.pone.0100090. eCollection 2014. PMID: 24937750 Free PMC Article</br>3:IC261 induces cell cycle arrest and apoptosis of human cancer cells via CK1δ/ɛ and Wnt/β-catenin independent inhibition of mitotic spindle formation. Cheong JK, Nguyen TH, Wang H, Tan P, Voorhoeve PM, Lee SH, Virshup DM.Oncogene. 2011 Jun 2;30(22):2558-69. doi: 10.1038/onc.2010.627. Epub 2011 Jan 24. PMID: 21258417 Free PMC Article</br>4:Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. Höttecke N, Liebeck M, Baumann K, Schubenel R, Winkler E, Steiner H, Schmidt B.Bioorg Med Chem Lett. 2010 May 1;20(9):2958-63. doi: 10.1016/j.bmcl.2010.02.110. Epub 2010 Mar 4. PMID: 20350806 </br>5:Anti-apoptotic and growth-stimulatory functions of CK1 delta and epsilon in ductal adenocarcinoma of the pancreas are inhibited by IC261 in vitro and in vivo. Brockschmidt C, Hirner H, Huber N, Eismann T, Hillenbrand A, Giamas G, Radunsky B, Ammerpohl O, Bohm B, Henne-Bruns D, Kalthoff H, Leithäuser F, Trauzold A, Knippschild U.Gut. 2008 Jun;57(6):799-806. doi: 10.1136/gut.2007.123695. Epub 2008 Jan 18. PMID: 18203806 </br>6: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 L, Milne DM, Stöter M, Deppert W, Campbell LE, Meek DW, Knippschild U.Oncogene. 2000 Nov 9;19(47):5303-13. PMID: 11103931 Free Article |
