TX-1123 may be useful as a therapeutic agent for cancer treatment in animal models. A cell-permeable, reversible and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as a kinase inhibitor for proto-oncogene tyrosine-protein kinase Src (c-Src, IC50 = 2.2 μM), eukaryotic elongation factor-2 kinase (eEF2-K, IC50 = 3.2 μM), and protein kinase A (PKA, IC50 = 9.6 μM). TX-1123 has been shown to inhibit EGFR-K and PKC, but only at much higher concentrations (IC50 = 320 μM).
Additionally, TX-1123 has been reported to exhibit potent anti-tumor activity in HepG2(EC50 = 3.66) and HCT116 (EC50 = 39 μM) tumor cells, with greatly reduced mitochondrial- (≥1000-fold) and hepato-toxicity (≥50-fold) when compared with another tyrphostin, AG 17 (sc-200568).
1. Hori, Hitoshi., et al., 2002. TX-1123: an antitumor 2-hydroxyarylidene-4-cyclopentene-1,3-dione as a protein tyrosine kinase inhibitor having low mitochondrial toxicity. Bioorganic & medicinal chemistry. 10(10): 3257-65. PMID: 12150871
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