TAK1 inhibitor
CAS：1315355-93-1
分子式：C29H30F3N5O2
分子量：537.58
纯度：98%
存储：Store at -20°C

Background:

NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
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]. NG25 is very potent suppressor of CpG B- or CpG A-stimulated secretion of IFNα and CL097-stimulated secretion of IFNβ, with complete inhibition by 400 nM[2]. NG25 treatment reduces cell viability of all tested breast cancer cell lines in a dose dependent manner. NG25 (2?μM) enhances the cytotoxic effect of Dox on breast cancer cells[3].
Reference:
[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.