|
TX-1123
2-((3,5-di-tert-Butyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione, PKA Inhibitor XII
A cell-permeable, reversible, and substrate-competitive 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.
产品信息
Form Yellow solid
Primary Target Src
Primary Target IC50 2.2 µM
Secondary target eEF2-K and PKA (IC50 = 3.2 and 9.6 µM, respectively), while it inhibits EGFR-K and PKC (IC50 = 320 µM)
Molar mass 312.4
Protect from Light 是的
Packaged under inert gas 是的
Cell permeable 是的
Purity ≥95% by HPLC
Solubility DMSO
Chemical formula C20H24O3
CAS number 157397-06-3
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Harmful |