IC261

• CAT Number: I002409
• CAS Number: 186611-52-9
• Molecular Formula: C₁₈H₁₇NO₄
• Molecular Weight: 311.34
• Purity: ≥95%
• Synonyms: (E)-3-(2,4,6-trimethoxybenzylidene)indolin-2-one
• Target: CK1
• Solubility: DMSO: ≥ 33 mg/mL
• Storage: Store at -20°C
• IC50: 16 μM [2]
• 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)
• InChIKey: JBJYTZXCZDNOJW-UHFFFAOYSA-N
• SMILES: COC1=CC(=C(C(=C1)OC)C=C2C3=CC=CC=C3NC2=O)OC

IC261(CAT: I002409)is indeed a novel inhibitor of casein kinase 1 (CK1). It has been shown to activate the mitotic checkpoint control by inhibiting CK1 activity, leading to cell cycle arrest at the G2/M phase. By interfering with CK1-mediated phosphorylation events, IC261 disrupts critical cellular processes regulated by CK1, such as cell division, circadian rhythm, and Wnt signaling. Its ability to modulate CK1 activity makes it a valuable tool in research aimed at understanding CK1 signaling pathways and exploring potential therapeutic applications in various diseases.

Reference

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 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 Article3: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 Article4: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 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 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