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.

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₁₄H₁₂O₃S₂
• Numer CAS: 213261-59-7
• Masa cząsteczkowa: 292.37
• MDL number: MFCD03235294
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥97% (HPLC)
• Form: crystalline solid
• Storage condition: OK to freeze, protect from light

Właściwości

• Quality Segment: 100
• assay: ≥97% (HPLC)
• form: crystalline solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• solubility: ethanol: 1 mg/mL, DMSO: 3 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: [s]1c(ccc1c2[o]c(cc2)c3[s]c(cc3)CO)CO
• 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
• InChI key: KZENBFUSKMWCJF-UHFFFAOYSA-N

Opis

General description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
p53

Product does not compete with ATP.

Reversible: no

Packaging

Packaged under inert gas

Preparation Note

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

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.

Legal Information

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

Disclaimer

Toxicity: Irritant (B)

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• Co się dzieje?: WGK 1
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable