Description |
InvivoChem Cat #:V4593CAS #:1111556-37-6Purity >=98%Description: Takinib is a novel, potent and selective TAK1 inhibitor with an IC50 of 9.5 nM. Takinib induces apoptosis following TNF-alpha stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is an inhibitor of autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation. Overall, Takinib is an attractive starting point for the development of inhibitors that sensitize cells to TNF-alpha-induced cell death, with general implications for cancer and autoimmune disease treatment. Tumor necrosis factor alpha (TNF-alpha) has both positive and negative roles in human disease. In certain cancers, TNF-alpha is infused locally to promote tumor regression, but dose-limiting inflammatory effects limit broader utility. In autoimmune disease, anti-TNF-alpha antibodies control inflammation in most patients, but these benefits are offset during chronic treatment. TAK1 acts as a key mediator between survival and cell death in TNF-alpha-mediated signaling. References: Cell Chem Biol. 2017 Aug 17; 24(8):1029-1039.
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Name: Takinib CAS#: 1111556-37-6 Chemical Formula: C18H18N4O2 Exact Mass: 322.143 Molecular Weight: 322.36 Elemental Analysis: C, 67.07; H, 5.63; N, 17.38; O, 9.93 |
Technical Information |
Synonym: EDHS-206; EDHS 206; EDHS206 IUPAC/Chemical Name: 3-N-(1-Propylbenzimidazol-2-yl)benzene-1, 3-dicarboxamide InChi Key: UOZVVPXKJGOFIG-UHFFFAOYSA-N InChi Code: InChI=1S/C18H18N4O2/c1-2-10-22-15-9-4-3-8-14(15)20-18(22)21-17(24)13-7-5-6-12(11-13)16(19)23/h3-9, 11H, 2, 10H2, 1H3, (H2, 19, 23)(H, 20, 21, 24) SMILES Code: O=C(C1=CC=CC(C(NC2=NC3=CC=CC=C3N2CCC)=O)=C1)N |