IC261 is a casein kinase 1 δ (CK1δ) and CK1 ε inhibitor. IC261 induces cell cycle arrest and apoptosis of human cancer cells via CK1δ/ɛ and Wnt/β-catenin independent inhibition of mitotic spindle formation.
1: Föhr KJ, Knippschild U, Herkommer A, Fauler M, Peifer C, Georgieff M, Adolph O. State-dependent block of voltage-gated sodium channels by the casein-kinase 1 inhibitor IC261. Invest New Drugs. 2017 Feb 6. doi: 10.1007/s10637-017-0429-0. [Epub ahead of print] PubMed PMID: 28164251.
2: Stöter M, Krüger M, Banting G, Henne-Bruns D, Knippschild U. Microtubules depolymerization caused by the CK1 inhibitor IC261 may be not mediated by CK1 blockage. PLoS One. 2014 Jun 17;9(6):e100090. doi: 10.1371/journal.pone.0100090. PubMed PMID: 24937750; PubMed Central PMCID: PMC4061085.
3: Cheong JK, Nguyen TH, Wang H, Tan P, Voorhoeve PM, Lee SH, Virshup DM. IC261 induces cell cycle arrest and apoptosis of human cancer cells via CK1δ/ɛ and Wnt/β-catenin independent inhibition of mitotic spindle formation. Oncogene. 2011 Jun 2;30(22):2558-69. doi: 10.1038/onc.2010.627. PubMed PMID: 21258417; PubMed Central PMCID: PMC3109269.
4: Höttecke N, Liebeck M, Baumann K, Schubenel R, Winkler E, Steiner H, Schmidt B. Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. Bioorg Med Chem Lett. 2010 May 1;20(9):2958-63. doi: 10.1016/j.bmcl.2010.02.110. PubMed PMID: 20350806.
5: 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. 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. Gut. 2008 Jun;57(6):799-806. doi: 10.1136/gut.2007.123695. PubMed PMID: 18203806.
6: Behrend L, Milne DM, Stöter M, Deppert W, Campbell LE, Meek DW, Knippschild U. 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. 2000 Nov 9;19(47):5303-13. PubMed PMID: 11103931.
Chemical |
CAS Num |
186611-52-9 |
Chemical Formula |
C18H17NO4 |
Molecular Weight |
311.34 |
IUPAC Chemical Name |
3-[(2,4,6-trimethoxyphenyl)methylidene]-2,3-dihydro-1H-indol-2-one |
Exact Mass |
311.1158 |
Elemental Analysis |
C, 69.44; H, 5.50; N, 4.50; O, 20.56 |
Synonym |
IC261; IC-261; IC 261. |
Solubility |
Soluble in DMSO |
SMILES Code |
O=C1NC2=C(C=CC=C2)/C1=C\C3=C(OC)C=C(OC)C=C3OC |
Biological |
Targets and Effects |
N/A |
Pathways |
Apoptosis |
Physical |
Appearance |
Solid powder |
Purity |
>98% (or refer to the Certificate of Analysis) |
Shipping Condition |
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
Storage Condition |
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Shelf Life |
>2 years if stored properly |