GAK inhibitor 49

产品说明书

Print
Chemical Structure| 319492-82-5 同义名 : -
CAS号 : 319492-82-5
货号 : A1359459
分子式 : C20H22N2O5
纯度 : 99%+
分子量 : 370.4
MDL号 : MFCD29701419
存储条件：

Pure form Keep in dark place, sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(134.99 mM)，配合低频超声，并水浴加热至45℃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 Cyclin G associated kinase (GAK) is a ubiquitously expressed 160 kDa serine/threonine kinase involved in membrane trafficking. GAK inhibitor 49 is a potent, selective and ATP-competitive GAK inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 shows a weak inhibitory effect on AAK1, BMP2K and STK16, with IC50s of 28, 63 and >100 μM, respectively[1].
作用机制 GAK inhibitor 49 was docked into the active site of the GAK[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.70mL

0.54mL

0.27mL

13.50mL

2.70mL

1.35mL

27.00mL

5.40mL

2.70mL
参考文献

[1]Asquith CRM, et al. Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase. Chem Med Chem. 2018 Jan 8;13(1):48-66