For research use only. Not for therapeutic Use.
NG-25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1. It also inhibits the Src family kinases Src and LYN and Abl family kinases as well as CSK, FER, and p38α. NG 25 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. NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner. It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12D mouse orthotopic model of colorectal cancer.
| Catalog Number | I033234 |
| CAS Number | 2108554-00-1 |
| Synonyms | NG-25 HCl; NG-25 Hydrochloride; NG-25 trihydrochloride; NG-25; NG25; NG 25; |
| Molecular Formula | C29H33Cl3F3N5O2 |
| Purity | 98% |
| Target | MAP3K |
| Solubility | Soluble in DMSO |
| Appearance | Solid powder |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| IUPAC Name | N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-3-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)-benzamide, trihydrochloride. |
| InChI | InChI=1S/C29H30F3N5O2.3ClH/c1-3-36-12-14-37(15-13-36)18-21-6-7-22(17-24(21)29(30,31)32)35-28(38)20-5-4-19(2)26(16-20)39-25-9-11-34-27-23(25)8-10-33-27;;;/h4-11,16-17H,3,12-15,18H2,1-2H3,(H,33,34)(H,35,38);3*1H |
| InChIKey | QOIOJVPRHIAONM-UHFFFAOYSA-N |
| SMILES | [H]Cl.[H]Cl.[H]Cl.O=C(NC1=CC=C(CN2CCN(CC)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(OC4=C5C(NC=C5)=NC=C4)=C3 |
| Reference | 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). |
