货号:A1000438 同义名: CP 43;Compound 43 TAO Kinase Inhibitor
TAO Kinase inhibitor 1是一种选择性的ATP竞争性TAOK激酶抑制剂,对TAOK1(IC50 11 nM)和TAOK2(IC50 15 nM)具有较强的抑制作用,能延迟有丝分裂并增加SKBR3乳腺癌细胞系中的有丝分裂细胞死亡。
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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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 850467-66-2 |
分子式 | C25H24N2O2 |
分子量 | 384.47 |
别名 | CP 43;Compound 43 TAO Kinase Inhibitor |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,Room Temperature |
溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |