Molecular structure of IC261, CAS Number: 186611-52-9
IC261 (CAS 186611-52-9)
See product citations (11)
Alternate Names:
SU5607
Application:
IC261 is a selective casein kinase 1δ and 1ε inhibitor
CAS Number:
186611-52-9
Purity:
≥95%
Molecular Weight:
311.3
Molecular Formula:
C18H17NO4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Shown to inhibit casein kinase 1δ (IC50 = 0.7-1.3 μM), and casein kinase 1ε (IC50 = 0.6-1.4 μM). Inhibition is reversible and in a competitive manner with respect to ATP. IC261 also has been shown to weakly inhibit casein kinase 1α1 (IC50 = 11-21 μM), PKA, cdc2 p34, and Fyn (p55). Immunofluorescence images indicate that IC261 causes multipolar mitosis through centrosome amplification. IC261 allows for selective inhibition of casein kinase 1δ and 1ε, which can help to elucidate key aspects of cell division.
IC261 (CAS 186611-52-9) References
- Crystal structure of a conformation-selective casein kinase-1 inhibitor. | Mashhoon, N., et al. 2000. J Biol Chem. 275: 20052-60. PMID: 10749871
- 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., et al. 2000. Oncogene. 19: 5303-13. PMID: 11103931
- Wnt-5a-CKI{alpha} signaling promotes {beta}-catenin/E-cadherin complex formation and intercellular adhesion in human breast epithelial cells. | Medrek, C., et al. 2009. J Biol Chem. 284: 10968-79. PMID: 19244247
- Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. | Höttecke, N., et al. 2010. Bioorg Med Chem Lett. 20: 2958-63. PMID: 20350806
- 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., et al. 2011. Oncogene. 30: 2558-69. PMID: 21258417
- Microtubules depolymerization caused by the CK1 inhibitor IC261 may be not mediated by CK1 blockage. | Stöter, M., et al. 2014. PLoS One. 9: e100090. PMID: 24937750
- State-dependent block of voltage-gated sodium channels by the casein-kinase 1 inhibitor IC261. | Föhr, KJ., et al. 2017. Invest New Drugs. 35: 277-289. PMID: 28164251
- IC261 suppresses progression of hepatocellular carcinoma in a casein kinase 1 δ/ε independent manner. | Yuan, F., et al. 2020. Biochem Biophys Res Commun. 523: 809-815. PMID: 31954519
- IC261, a specific inhibitor of CK1δ/ε, promotes aerobic glycolysis through p53-dependent mechanisms in colon cancer. | Liu, M., et al. 2020. Int J Biol Sci. 16: 882-892. PMID: 32071557
- A Rationale for Drug Design Provided by Co-Crystal Structure of IC261 in Complex with Tubulin. | Xian, J., et al. 2021. Molecules. 26: PMID: 33579052
Inhibitor of:
β-Arrestin-1, APMSF, CaMKKβ, Casein Kinase, casein kinase I delta, casein kinase I epsilon, casein kinase Iα, casein kinase Iδ, casein kinase Iγ1, casein kinase Iγ2, casein kinase Iγ3, CELSR1, CSNK1A1L, Dyrk1A, HR, LOC100041343, Neudesin, Nlk, PCDH11X, Prickle1, Ser/Thr Protein Kinase, Snurportin-1, and Type I 4-phosphatase.Activator of:
CLK3, and GEMC1.Substrate of:
LTC4 synthase.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
IC261, 5 mg | sc-3561 | 5 mg | $140.00 |