产品说明书

NG25

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Chemical Structure| 1315355-93-1 同义名 : -
CAS号 : 1315355-93-1
货号 : A493735
分子式 : C29H30F3N5O2
纯度 : 99%+
分子量 : 537.576
MDL号 : MFCD19443255
存储条件:

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 16 mg/mL(29.76 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 NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively. NG25 also potently suppresses several kinases such as LYN, CSK, FER, p38α, ABL,ARG and SRC, with IC50s of 12.9, 56.4, 82.3, 102, 75.2, and 113 nM, respectively[1]. NG25fully blocks CpG B- or CpG A-induced IFNα secretion and CL097-induced IFNβ secretion at a concentration of 400 nM[2]. Furthermore, NG25 decreases the viability of various breast cancer cell lines in a dose-dependent manner, and at a concentration of 2 μM, it enhances the cytotoxic effects of Doxorubicin on these cells[3].
作用机制 NG25 may bind to the ATP binding pocket of TAK1.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.86mL

0.37mL

0.19mL

9.30mL

1.86mL

0.93mL

18.60mL

3.72mL

1.86mL

参考文献

[1]Tan L, et al. Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J Med Chem. 2015 Jan 8;58(1):183-96.

[2]Pauls E, et al. Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cells. J Biol Chem. 2012 Jun 1;287(23):19216-28.

[3]Wang Z, et al. TAK1 inhibitor NG25 enhances doxorubicin-mediated apoptosis in breast cancer cells. Sci Rep. 2016 Sep 7;6:32737.