tak-1-in-2

TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM[1]. TAK1-IN-2 (compound 54) (10 μM) has no effect on cell viability in TNF-α stimulated HCT-15 cells[1]. [1]. Veerman JJN, et, al. Discovery of 2,4-1 H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors. ACS Med Chem Lett. 2021 Mar 3;12(4):555-562.

(5E)-7-Oxozeaenol is a resorcylic acid lactone that has been found in the fungus MSX 63935 and has enzyme inhibitory and anticancer activities.1,2 It inhibits TGF-β-activated kinase 1 (TAK-1; IC50 = 1.3 μM).1 (5E)-7-Oxozeaenol inhibits proliferation of MCF-7, H460, SF-268, HT-29, and MDA-MB-435 human cancer cells with IC50 values of 4.9, 1.2, 5.6, 4.4, and 5.5 μM, respectively.2 |1. Fakhouri, L., El-Elimat, T., Hurst, D.P., et al. Isolation, semisynthesis, covalent docking and transforming growth factor beta-activated kinase 1 (TAK1)-inhibitory activities of (5Z)-7-oxozeaenol analogues. Bioorg. Med. Chem. 23(21), 6993-6999 (2015).|2. Ayers, S., Graf, T.N., Adcock, A.F., et al. Resorcylic acid lactones with cytotoxic and NF-κB inhibitory activities and their structure-activity relationships. J. Nat. Prod. 74(5), 1126-1131 (2011).

Modakafusp alfa (TAK-573) 是一种融合蛋白，由人源化抗CD38 IgG4 单克隆抗体和2个减毒IFNα2b分子组成。该化合物主要用于多发性骨髓瘤的研究。

Firazorexton hydrate (TAK-994)为一种高效的食欲素2型受体(OX2R)激动剂，EC50值为19 nM。在发作性睡病小鼠模型中，该化合物能够有效减少觉醒碎片和猝倒样发作的发生。