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CAS No.: 2109805-56-1

CLK-IN-T3 Catalog No. CSN20276

Synonyms: T3;CLK Inhibitor T3;T3-CLK

Clk inhibitor T3 is a highly selective, stable CLK inhibitor with high specificity to CLK1-3 protein isoforms.

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技术信息

生物活性

描述Cyclin-dependent kinases (CDKs) are a group of multifunctional enzymes consisting of catalytic and regulatory subunits. The regulatory subunit, cyclin, remains dissociated under normal circumstances, and complexation of cyclin with the catalytic subunit of CDK leads to its activation for phosphorylation of protein substrates^[2]. CDKs are activated by cyclins, which play important roles in dictating the actions of CDK/cyclin complexes. Cyclin binding influences the substrate specificity of these complexes in addition to their susceptibility to inhibition or degradation. CDK/cyclin complexes are best known to promote cell cycle progression in the mitotic cell cycle but are also crucial for important cellular processes not strictly associated with cellular division^[3]. CLK-IN-T3 is a potent inhibitor of CDC-like kinase (CLK) (IC50s: 0.67 nM, 15 nM, and 110 nM for CLK1, CLK2, and CLK3 protein kinases) with anti-cancer activity. CLK-IN-T3 (0.5-1.0 µM; 6 hours) reduces phosphorylation of CLK-targeted SR proteins and CLK proteins increase slightly. CLK-IN-T3 (0.1-10.0 µM; 24 hours) causes mild cell cycle arrest at the G2/M boundary with long-duration (24 h). CLK-IN-T3 has IC50s of 260 nM and 230 nM for DYRK1A and DYRK1B, respectively^[4].In embryonic cells, cardiomyocytes, and hearts, the growth and heart rates were significantly slowed in clk-1(-/-) compared with wild-type or heterozygous mouse tissues. Moreover, frequent apoptosis and a significant reduction in mitochondrial functions, including membrane potential and ATP production, were observed in the clk-1(-/-) cells and hearts^[5].
参考文献

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
- 2.0722 mL
- 10.3610 mL
- 20.7221 mL
- 5 mM
- 0.4144 mL
- 2.0722 mL
- 4.1444 mL
- 10 mM
- 0.2072 mL
- 1.0361 mL
- 2.0722 mL

技术信息

CAS号	2109805-56-1	储存条件	粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C28H30N6O2	运输	蓝冰
分子量	482.58	别名	T3;CLK Inhibitor T3;T3-CLK;MDK-5561

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