506149

p53 Activator III, RITA

The p53 Activator III, RITA, also referenced under CAS 213261-59-7, modulates the biological activity of p53. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

• Synonyme(s) : p53 Activator III, RITA, NSC 652287, 2,5- bis-(5-Hydroxymethyl-2-thienyl)-furan, Reactivation of p53 and Induction of Tumor cell Apoptosis, MDM2 Antagonist VII, MDM2 Inhibitor X
• Formule empirique (notation de Hill): C₁₄H₁₂O₃S₂
• Numéro CAS: 213261-59-7
• Poids moléculaire : 292.37
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥97% (HPLC)
• Forme: crystalline solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Solubilité: ethanol: 1 mg/mL; DMSO: 3 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• InChI: 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
• Clé InChI: KZENBFUSKMWCJF-UHFFFAOYSA-N

Description

Description générale

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.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
p53

Product does not compete with ATP.

Reversible: no

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Irritant (B)

Reconstitution

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

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable