TX-1918 may be useful as a therapeutic agent for cancer treatment in animal models. A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eukaryotic elongation factor-2 kinase (eEF2K, IC50 = 440 nM). At higher concentrations, TX-1918 has been shown to inhibit other kinases, including proto-oncogene tyrosine-protein kinase Src (c-SRC, IC50 = 4.4 μM), protein kinase A and C (PKA and PKC, IC50 = 44 μM for each), and epidermal growth factor receptor kinase (EGFR-K, IC50 = 440 μM).
Additionally, TX-1918 has been reported to exhibit potent anti-tumor activity in HepG2 (EC50 = 2.07) and HCT116 (EC50 = 230 μM) tumor cells, with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-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
See how others have used TX-1918 (CAS 503473-32-3). Click on the entry to view the PubMed entry .
PMID: # 33662272 Shen, Y.|Zhang, ZC.|Cheng, S.|Liu, A.|Zuo, J.|Xia, S.|Liu, X.|Liu, W.|Jia, Z.|Xie, W.|Han, J.| et al. 2021. Mol Cell. 81: 1425-1438.e10.