TX-1918 is a cell-permeable tyrphostin derivative that inhibits eukaryotic elongation factor-2 kinase (eEF-2K; IC50 = 440 nM). It inhibits Src, PKA, PKC, and EGFR kinases at much higher concentrations (IC50s = 4.4, 44, 44, and 440 uM, respectively). TX-1918 disrupts the proliferation of HepG2 and HCT116 tumor cells (EC50s = 2.07 and 230 uM, respectively) with >=5,000-fold and >=90-fold reduced mitochondrial- and hepato-toxicity, respectively when compared with the tyrphostin AG-17 [1]
Reference:
[1]. Hori, H., Nagasawa, H., Ishibashi, M., et al. TX-1123: An antitumor 2-hydroxyarylidene-4-cyclopentene-1,3-dione as a protein tyrosine kinase inhibitor having low mitochondrial toxicity. Bioor. Med. Chem. Lett. 10(10), 3257-3265 (2002).