(E/Z)-TG003

(E/Z)-TG003 是一种有效的 ATP 竞争性 Cdc2 样激酶 (Clk) 抑制剂,抑制 Clk1 和 Clk4 的 IC50值分别为 20 和 15 nM。它是 (Z)-TG003 和 (E)-TG003的消旋体。

CAS号

300801-52-9

分子式

C13H15NO2S

主要靶点

BCL|CDK

仅限科研使用

Cat No : CM03355

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Synonyms

TG003



产品信息

(E/Z)-TG003 is a potent and ATP-competitive Cdc2-like kinase (Clk) inhibitor.

CAS号 300801-52-9
分子式 C13H15NO2S
主要靶点 BCL|CDK
主要通路 凋亡|细胞周期
分子量 249.33
纯度 98.73%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 TG003

靶点活性

mCLK4:15 nM|mCLK1:20 nM|mCLK2:200 nM

体内活性

TG003通过抑制IL-1β异核RNA的剪接阻断血小板产生IL-1β RNA。在3T3-L1脂肪细胞分化过程中,TG003也阻断PKCβII的可变剪接和PPARγ1和PPARγ2的表达。TG003通过抑制Clk1/Sty介导的磷酸化抑制人类β珠蛋白在体外的SF2/ASF依赖性剪接。TG003抑制哺乳动物细胞中Clk1/Sty激酶活性,而对10 μM浓度的HeLa和COS-7细胞的生长没有毒性作用。

体外活性

10 μM TG003能够治疗非洲爪蟾体内过度Clk活性诱导的胚胎缺陷.

溶解度

Ethanol:<1 mg/mL,DMSO:6 mg/mL (24.06 mM),warmed

细胞实验

2 × 105 HeLa cells or 1.5 × 105 COS-7 cells resuspended in 2 mL of medium are plated on 6-well dishes, and 2 μL of 10 mM TG003 dissolved in Me2SO (final concentration at 10 μM), or 2 μL of Me2SO, is added to some wells. Cells are trypsinized, and the density is counted every 24 h for 3 days. Cells are then fixed with 1 mL of ice-cold 70% ethanol, washed with PBS, incubated in 1 ml of PBS containing 1 μg/mL DNase-free RNase A and 50 μg/mL propidium iodide for 20 min at 37 °C, and proceeded to cell cycle analysis by FACSCalibur.(Only for Reference)

参考文献

1.Muraki M, et al. J Biol Chem. 2004, 279(23), 24246-24254.
2.Brown GT, et al. J Immunol. 2011, 186(9), 5489-5496.
3.Li P, et al. PLoS One. 2013, 8(1), e53268.

The molarity calculator equation

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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