NG25 is a novel inhibitor of TAK1 with enzymatic IC50s of 149 and 21.7 nM for TAK1 and MAP4K2 respectively.
Targets
TAK1 [1]()
MAP4K2 [1]()
In vitro
NG25 can inhibit phosphorylation of proteins predicted to be downstream of TAK1 and MAP4K2 such as IKK, p38 and JNK at concentrations of less than 100 nM[1].
Assay
Methods
Test Index
PMID
Western blot
p-p38 / p38 / IκBα ;
PubMed: 27599572
Breast cancer cell lines T-47D, MCF7, HCC1954, MDA-MB-231, and BT-549 were treated with Dox (20 μM) alone or combined with NG25 (2 μM) for 0, 2 h, 4 h or 6 h. The protein extracts were subjected to SDS-PAGE and immunoblotted with the antibodies against p-p38, p38, and IκBα. β-actin were detected as loading controls for whole cell extracts.
27599572
Growth inhibition assay
Cell viability ;
PubMed: 27599572
(a) Cytotoxic effect of NG25 on breast cancer cells in CCK-8 assay. Five human breast cancer cell lines T-47D, MCF7, HCC1954, MDA-MB-231, and BT-549 were treated with NG25 at 0, 1 μM, 2 μM, 5 μM, 10 μM, and 20 μM for 72 h, then subjected to a CCK-8 assay. The absorbance of each well was measured at 450 nm and plotted for the cell viability curve. The data are represented as mean ± SD.Pvalues < 0.01 (**) or < 0.001 (***) were indicated. (b) IC50 values of NG25 in breast cancer cell lines were listed.
