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(E/Z)-TG003

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Chemical Structure| 300801-52-9 同义名 : TG003
CAS号 : 300801-52-9
货号 : A789987
分子式 : C13H15NO2S
纯度 : 99%+
分子量 : 249.329
MDL号 : MFCD00624584
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • CLK

    mCLK1, IC50:200 nM

    mCLK4, IC50:15 nM
描述 The Clk (Cdc2-like kinase) family, consisting of at least four members, has been implicated in regulating alternative splicing by phosphorylation of SR (serine/arginine-rich) proteins. TG003 is a potent and ATP-competitive inhibitor of Clk with IC50s of 15, 20, 200 nM for mClK4, mClK1 and mClK2, respectively. TG003 (1 μM; 4 h) inhibited SF2/ASF-dependent splicing in HeLa cytosolic S100 extract by suppression of Clk1/Sty-mediated phosphorylation. It attenuated the splicing of β-globin pre-mRNA in S100 extract complemented with rSF2/ASF. When treated with 10 μM TG003 for 12 hours, HA-Clk1/Sty was localized in nuclear speckles in HA-Clk1/Sty-overexpressing HeLa cells with suppressed phosphorylation of SR proteins. In vivo, the abnormal development phenotype of the Xenopus embryos was rescued when they were incubated with 10 μM TG003[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human STO cells Function assay Modulation of Clk/sty pre-mRNA splicing in human STO cells assessed as concentration required to increase in mature Clk2 mRNA level by RT-PCR analysis, EC50=6.6 μM 25221649
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.01mL

0.80mL

0.40mL

20.05mL

4.01mL

2.01mL

40.11mL

8.02mL

4.01mL
参考文献

[1]Muraki M, Ohkawara B, Hosoya T, et al. Manipulation of alternative splicing by a newly developed inhibitor of Clks. J Biol Chem. 2004;279(23):24246-54.

[2]Muraki M, et al. Manipulation of alternative splicing by a newly developed inhibitor of Clks. J Biol Chem. 2004 Jun 4;279(23):24246-54