IC261
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货号：A267194
同义名：
SU5607
IC261 is an ATP-competitive inhibitor of CK1 with IC50s about 1 μM for CK1δ and CK1ε, 16 μM for CK1α.
IC261 化学结构
IC261 3D分子结构
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价格
会员价
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IC261 纯度/质量文件 产品仅供科研
货号：A267194
标准纯度：
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产品说明书
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IC261 质控信息
PF-670462 2HCl
++++
CK1ε, IC50: 90 nM
CK1δ, IC50: 13 nM
99%+
D4476
++
CK1 from Schizosaccharomyces pombe, IC50: 200 nM
CK1δ, IC50: 300 nM
98%
SR-3029
+++
CK1ε, IC50: 260 nM
CK1δ, IC50: 44 nM
99%+
IWP-2
+++
Wnt
98%
LY364947
++
98%
TA-01
++++
CK1ε, IC50: 6.4 nM
CK1δ, IC50: 6.8 nM
p38 MAPK
99%+
IC261
+
98%
PF-4800567
+++
casein kinase 1 epsilon, IC50: 32 nM
casein kinase 1 delta, IC50: 711 nM
99%+
CK1-IN-1
++++
CK1ε, IC50: 16 nM
CK1δ, IC50: 15 nM
98%
Longdaysin
+
CKIα, IC50: 5.6 μM
CKIδ, IC50: 8.8 μM
99%+
Silmitasertib
++++
99%+
Ellagic acid (hydrate)
+++
PKA
95+%
DMAT
+++
98%
Hematein
++
98+%
Silmitasertib sodium salt
++++
CK2α', IC50: 1 nM
CK2α, IC50: 1 nM
99%+
LY294002
+++
99%+
A-3 HCl
+
++
MLCK,PKA,PKC
98+%
TBB
+
++
98%
TTP 22
++
98%+
DRB
✔
99%+
BioE-1115
+
99%+
(E/Z)-GO289
++++
99%+
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
IC261 生物活性
靶点
描述
IC261 is a novel inhibitor of CK1 for isoforms of α[5] [6] [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]
IC261 动物研究
Dose
Mice: 30 mg/kg[4]
Administration
i.p.
IC261 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.
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IC261 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
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
IC261 技术信息
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