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.

• Sinonimo/i: 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
• Formula empirica (notazione di Hill): C₁₄H₁₂O₃S₂
• Numero CAS: 213261-59-7
• Peso molecolare: 292.37
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥97% (HPLC)
• Forma fisica: crystalline solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Solubilità: ethanol: 1 mg/mL; DMSO: 3 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 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; KZENBFUSKMWCJF-UHFFFAOYSA-N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
p53

Product does not compete with ATP.

Reversible: no

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Irritant (B)

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable