850467-66-2|TAO Kinase inhibitor 1|CsnPharm

CAS No.: 850467-66-2

TAO Kinase inhibitor 1 Catalog No. CSN26245

Synonyms: CP 43;Compound 43 TAO Kinase Inhibitor

TAO Kinase inhibitor 1 is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. It inhibits TAOK phosphorylation and activation of JNK in vitro, and also prolongs duration of mitosis and increases mitotic cell death in the SKBR3 breast cancer cell line.

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400-920-2911

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技术信息

生物活性

描述The TAO (for thousand-and-one amino acids) protein kinases activate p38 mitogen-activated protein (MAP) kinase cascades in vitro and in cells by phosphorylating the MAP/ERK kinases (MEKs) 3 and 6. TAO protein kinases relay signals from carbachol through heterotrimeric G proteins to the p38 MAP kinase, which then activates TCFs in the nucleus^[1]. TAO Kinase inhibitor 1 is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively^[2]. TAO inhibitor 1 reduced tau phosphorylation on T123 and T427 (Identified in AD brains) and also on additional pathological sites (S262/S356 and S202/T205/S208) in vitro and in cell models. It is also decreased tau phosphorylation in differentiated primary cortial neurons without affecting markers of synapse and neuron health. Furthermore, the activity of TAOK decreased tau phosphorylation in induced pluripotent stem cell derived neurons from FTLD patients, as well as cortical neurons from a transgenic mouse model of tauopathy (Tau3 mice)^[3].
参考文献

[1] Zhu Chen,et al. TAO (thousand-and-one amino acid) protein kinases mediate signaling from carbachol to p38 mitogen-activated protein kinase and ternary complex factors. J Biol Chem. 2003. 278(25), 22278-83.
[2] Chuay-Yeng Koo,et al. Targeting TAO Kinases Using a New Inhibitor Compound Delays Mitosis and Induces Mitotic Cell Death in Centrosome Amplified Breast Cancer Cells. Mol Cancer Ther. 2017. 16(1), 2410-2421.
[3] Giacomini, C., Koo, C.Y., Yankova, N. et al. A new TAOO kinase inhibitor reduces tau phosphorylation at sites associated with neurodegeneration in human tauopathies. Acta neuropahtol commun. 2018. 37(6).

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
- 2.6010 mL
- 13.0049 mL
- 26.0098 mL
- 5 mM
- 0.5202 mL
- 2.6010 mL
- 5.2020 mL
- 10 mM
- 0.2601 mL
- 1.3005 mL
- 2.6010 mL

技术信息

CAS号	850467-66-2	储存条件	粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C25H24N2O2	运输	蓝冰
分子量	384.47	别名	CP 43;Compound 43 TAO Kinase Inhibitor

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