tak1-in-3

TAK1-IN-3 是一种新型 ATP 竞争性 TAK1 抑制剂，可用于研究癌症。

NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively, in Gen2.2 cells in a concentration-dependent manner.2NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner.3It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12Dmouse orthotopic model of colorectal cancer. 1.Tan, L., Nomanbhoy, T., Gurbani, D., 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.58(1)183-196(2015) 2.Pauls, E., Shpiro, N., Peggie, M., et al.Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cellsJ. Biol. Chem. 287(23)19216-19228(2012) 3.Ma, Q., Gu, L., Liao, S., et al.NG25, a novel inhibitor of TAK1, suppresses KRAS-mutant colorectal cancer growth in vitro and in vivoApoptosis24(1-2)83-94(2019)

IRAK4-IN-22 是选择性的、口服具有活力的、强效的 IRAK4 抑制剂，能够作用于 IRAK4 (IC50: 3 nM) 和 TAK1 (IC50: 17 nM)。IRAK4-IN-21 对 IL-23 的产生表现出有效的抑制作用，其 IC50值为0.10 μM。IRAK4-IN-21 能够用于研究自身免疫性疾病，如斑块状银屑病和银屑病关节炎。

Triptriolide 通过调节Bcl-2家族蛋白并抑制Caspase-3来抑制Puromycin aminonucleoside [PAN] 诱导的小鼠足细胞凋亡 (apoptosis)。此外，Triptriolide 通过激活TAK1-NF-κB信号通路以及上调足细胞蛋白 podocin，从而促进细胞存活，并保护和恢复足细胞功能。