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IC261 is most commonly known as an inhibitor of casein kinase 1. It has been shown to reduce pancreatic tumor cell growth in vitro and in vivo. In addition, it also inhibits sodium channels in human TsA cells. Furthermore, IC261 has also been found to inhibit microtubule polymerization. In inflammatory pain model mice, IC261 decreased the frequency and amplitude of spontaneous excitatory postsynaptic currents.
| Cas No. | 186611-52-9 |
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| Purity | ≥98% |
| Formula | C18H17NO4 |
| Formula Wt. | 311.12 |
| Chemical Name | (3E)-3-(2,4,6-Trimethoxybenzylidene)-1,3-dihydro-2H-indol-2-one |
| IUPAC Name | (3E)-3-[(2,4,6-trimethoxyphenyl)methylidene]-1H-indol-2-one |
| Synonym | SU5607 |
| Solubility | Soluble in DMSO (10 mg/ml). Insoluble in water. |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Fohr KJ, Knippschild U, Herkommer A, et al. State-dependent block of voltage-gated sodium channels by the casein-kinase 1 inhibitor IC261. Invest New Drugs. 2017 Feb 6. Epub ahead of print. PMID: 28164251.
Stoter M, Kruger M, Banting G, et al. Microtubules depolymerization caused by the CK1 inhibitor IC261 may be not mediated by CK1 blockage. PLoS One. 2014 Jun 17;9(6):e100090. PMID: 24937750.
Kurihara T, Sakurai E, Toyomoto M, et al. Alleviation of behavioral hypersensitivity in mouse models of inflammatory pain with two structurally different casein kinase 1 (CK1) inhibitors. Mol Pain. 2014 Mar 10;10:17. PMID: 24612480.
Cheong JK, Nguyen TH, Wang H, et al. IC261 induces cell cycle arrest and apoptosis of human cancer cells via CK1δ/ε and Wnt/β-catenin independent inhibition of mitotic spindle formation. Oncogene. 2011 Jun 2;30(22):2558-2569. PMID: 21256417.