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TAO Kinase inhibitor 1

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Chemical Structure| 850467-66-2 同义名 : CP 43;Compound 43 TAO Kinase Inhibitor
CAS号 : 850467-66-2
货号 : A1000438
分子式 : C25H24N2O2
纯度 : 99%+
分子量 : 384.47
MDL号 : MFCD15612807
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(156.06 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

13.00mL

2.60mL

1.30mL

26.01mL

5.20mL

2.60mL
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).