Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Cell permeable: yes

Primary Targetp53

General description

A cell-permeable, p53-targeting, tricyclic thiophene derivative that displays antitumor properties. Blocks p53R12;MDM2 interaction and p53 ubiquitination and induces p53-dependent apoptosis in tumor cells expressing wild-type p53. Shown to restore the tumor suppressor function of p53 by inducing its accumulation in HCT116 colon carcinoma cells (~0.1 µM) and in p53-positive SCID mice xenografted with HCT116 cells (0.1, 1 or 10 mg/kg, ip) in vivo.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Grinkevich, V., et al. 2005. Nat. Med.11, 1136.Krajewski, M., et al. 2005. Nat. Med.11, 1135.Issaeva, N., et al. 2004. Nat. Med.10, 1321.Nieves-Neira, W., et al. 1999. Mol. Pharmacol.56, 478.Rivera, M.I., et al. 1999. Biochem. Pharmacol.57, 1283.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Irritant (B)