货号:A1000438 同义名: 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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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 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Room Temperature |
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 |