2-((3,5-di-tert-Butyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as an inhibitor for Src, eEF2-K, and PKA (IC50 = 2.2, 3.2, and 9.6 µM, respectively), while it inhibits EGFR-K and PKC at much higher concentrations (IC50 = 320 µM). Displays potent antitumor activity (EC50 = 3.66 and 39 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥1000-fold) and hepato-toxicity (≥50-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). It is therefore a more promising candidate as a therapeutic agent for cancer treatment. Purity: ≥95% by HPLC. Ref.: Hori, H., et al. 2003. Cell. Mol. Biol. Lett. 8, 528. Hori, H., et al. 2002. Bioorg. Med. Chem. 10, 3257. |
