IC261

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Chemical Structure| 186611-52-9 同义名 : SU5607
CAS号 : 186611-52-9
货号 : A267194
分子式 : C18H17NO4
纯度 : 98%
分子量 : 311.33
MDL号 : MFCD00118156
存储条件：

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(112.42 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • CK1

    CK1, IC50:16 μM
描述 IC261 is a novel inhibitor of CK1 for isoforms of α[5] ,δ and ε. It inhibited cytokinesis causing a transient mitotic arrest and also led to centrosome amplification causing multipolar mitosis[6]. Inhibition of CK1 α by IC261 at concentration<300μM dose-dependently reduced LRRK2 phosphorylation at S935 and S910, as well as resulted a loss of 14-3-3 binding[5].
作用机制 IC261 is an ATP-competitive inhibitor and form a complex with the catalytic domain of fission yeast casein kinase-1. It stabilized casein kinase-1 in a conformation midway between nucleotide substrate liganded and nonliganded conformations.[4]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.21mL

0.64mL

0.32mL

16.06mL

3.21mL

1.61mL

32.12mL

6.42mL

3.21mL
参考文献

[1]Chia R, Haddock S, et al. Phosphorylation of LRRK2 by casein kinase 1α regulates trans-Golgi clustering via differential interaction with ARHGEF7. Nat Commun. 2014 Dec 15;5:5827.

[2]Behrend L, Milne DM, et al. 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.

[3]Mashhoon N, DeMaggio AJ, et al. Crystal structure of a conformation-selective casein kinase-1 inhibitor. J Biol Chem. 2000 Jun 30;275(26):20052-60.

[4]Mashhoon N, DeMaggio AJ, Tereshko V, Bergmeier SC, Egli M, Hoekstra MF, Kuret J. Crystal structure of a conformation-selective casein kinase-1 inhibitor. J Biol Chem. 2000 Jun 30;275(26):20052-60. doi: 10.1074/jbc.M001713200. PMID: 10749871.

[5]Chia R, Haddock S, Beilina A, Rudenko IN, Mamais A, Kaganovich A, Li Y, Kumaran R, Nalls MA, Cookson MR. Phosphorylation of LRRK2 by casein kinase 1α regulates trans-Golgi clustering via differential interaction with ARHGEF7. Nat Commun. 2014 Dec 15;5:5827. doi: 10.1038/ncomms6827. PMID: 25500533; PMCID: PMC4268884.

[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. doi: 10.1038/sj.onc.1203939. PMID: 11103931.