Biochem/physiol Actions
Target IC50: 2.2, 3.2, and 9.6 µM against Src, eEF2-K, and PKA, respectively
Reversible: yes
Product competes with ATP.
Primary TargetSrc
Cell permeable: yes
General description
A cell-permeable, reversible and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as a kinase inhibitor for Src, eEF2-K, and PKA (IC50 = 2.2, 3.2, and 9.6 µM, respectively). Inhibits EGFR-K and PKC only at much higher concentrations (IC50 = 320 µM). Reported to exhibit potent anti-tumor 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). 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 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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Hori, H., et al. 2003. Cell. Mol. Biol. Lett.8, 528.Hori, H., et al. 2002. Bioorg. Med. Chem.10, 3257.
Packaging
Packaged under inert gas
10 mg in Plastic ampoule
Reconstitution
Following reconstitution, aliquot and freeze (- 20°C). Stock solutions are stable for up to 3 months at -20°C.
Warning
Toxicity: Harmful (C)
This product has met the following criteria to qualify for the following awards: