p53 Activator III, RITA-CAS 213261-59-7-Calbiochem

C₁₄H₁₂O₃S₂

292.37

A cell-permeable, p53-targeting, tricyclic thiophene derivative that displays antitumor properties. Blocks p53—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.
A cell-permeable, p53-targeting, tricyclic thiophene derivative that displays antitumor properties. Blocks p53—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.

Cell permeable: yes
Primary Target
p53
Product does not compete with ATP.
Reversible: no

Toxicity: Irritant (B)

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

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.

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

100

≥97% (HPLC)

crystalline solid

Calbiochem^®

OK to freeze
protect from light

ethanol: 1 mg/mL
DMSO: 3 mg/mL

ambient

2-8℃

1S/C14H12O3S2/c15-7-9-1-5-13(18-9)11-3-4-12(17-11)14-6-2-10(8-16)19-14/h1-6,15-16H,7-8H2

KZENBFUSKMWCJF-UHFFFAOYSA-N

1 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 1