301836-43-1|D4476|CsnPharm

CAS No.: 301836-43-1

D4476 Catalog No. CSN13638

Synonyms: Casein Kinase I Inhibitor

D4476 is a potent, selective, and cell-permeant CK1 (casein kinase 1) inhibitor with IC50 of 200 nM and 300 nM in a cell-free assay for CK1 from Schizosaccharomyces pombe and CK1δ, respectively. Also acts as an ALK5 inhibitor with IC50 of 500 nM.

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400-920-2911

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生物活性

实验方案

技术信息

生物活性

描述D4476 is a dual inhibitor of both ALK5 with IC50 value of 94nM, and CK1 with IC50 values of 200nM and 300nM for CK1 and CK1δ from S. pombe, respectively^[1]^[2]. D4476 inhibited TGF-β1-induced (FN) mRNA formation in A498 cells with IC50 value of 0.05μM and significantly reduced the TGF-β1-induced nuclear accumulation of Smad proteins with an IC50 value of 0.04 µM^[1]. D4476 dose-dependently inhibited the phosphorylation of FOXO1a induced by insulin at Ser322 and Ser325 at concentration ranging in 25-150μM in H4IIE cells, but not the phosphorylation of Thr24, Ser256, Ser319 catalyzed by PKB, or the constitutively phosphorylated Ser329. Prior treatment with 150μM D4476 reduced the IGF-1 and serum-induced nuclear exclusion of FOXO1a to about 3 fold. This retarding of nuclear exclusion by D4476 may due to the acceleration of nuclear export^[2].
作用机制D4476 is an ATP-competitive inhibitor of CK1.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
A375 cells	10-80 μM	Function assay	48 h	Inhibition of CK1-MDM2 complex in human A375 cells assessed as increase in p21 protein level at 10 to 80 uM after 48 hrs by immunoblotting analysis	24007918

动物研究
剂量
Mice^[3] (i.p.): 15 mg/kg

给药途径
i.p.
参考文献

动物研究
剂量	Mice^[3] (i.p.): 15 mg/kg
给药途径	i.p.

[1] Callahan JF, Burgess JL, et al. Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5). J Med Chem. 2002 Feb 28;45(5):999-1001.
[2] Rena G, Bain J, et al. D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a. EMBO Rep. 2004 Jan;5(1):60-5.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5100 mL
- 12.5498 mL
- 25.0995 mL
- 5 mM
- 0.5020 mL
- 2.5100 mL
- 5.0199 mL
- 10 mM
- 0.2510 mL
- 1.2550 mL
- 2.5100 mL

技术信息

CAS号

301836-43-1

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H18N4O3

运输

蓝冰

分子量

398.41

别名

Casein Kinase I Inhibitor

溶解度

DMSO	50.0 mg/mL (125.5 mM)
Water	insoluble

动物实验配方

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