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TX-1918
2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione
A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC50 = 440 nM), while it inhibits other kinases at much higher concentrations (IC50 = 4.4, 44, 44, and 440 µM for Src, PKA, PKC, and EGFR-K, respectively). Displays potent antitumor activity (EC50 = 2.07 and 230 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-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.
产品信息
Form Light orange solid
Primary Target eEF2-K
Primary Target IC50 440 nM
Secondary target IC50 = 4.4, 44, 44, and 440 µM for Src, PKA, PKC, and EGFR-K, respectively
Molar mass 228.2
Protect from Light 是的
Packaged under inert gas 是的
Cell permeable 是的
Purity ≥95% by HPLC
Solubility DMSO
Chemical formula C14H12O3
CAS number 503473-32-3
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Harmful |