Cat. No. 2443
Alternative Name: NSC 652287
Chemical Name: 5,5'-(2,5-Furandiyl)bis-2-thiophenem
Biological ActivityAnti-tumor agent that binds wild-type p53 (Kd = 1.5 nM) preventing p53-MDM2 (HDM2) interaction. Induces p53 accumulation and stimulates apoptosis in tumor cell lines expressing wild-type p53 in vitro and in vivo. Inhibits HPV-E6-mediated proteasomal degradation. Suppresses expression of cervical carcinoma HeLa xenografts in vivo.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Rivera et al (1999) Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines: differential accumulation and metabolism. Biochem.Pharmacol. 57 1283. PMID: 10230772.
Issaeva et al (2004) Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumours. Nature Med. 10 1321.
Espinoza-Fonseca (2005) Targeting MDM2 by the small molecule RITA: towards the development of new multi-target drugs against cancer. Theor.Biol.Med.Mod. 2 38.
Zhao et al (2010) Rescue of p53 function by small-molecule RITA in cervical carcinoma by blocking E6-mediated degradation. Cancer Res. 70 3372. PMID: 20395210.
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Keywords: RITA, supplier, p53-MDM2, interaction, inhibitors, antitumor, agent, MDM2-p53, MDM2, p14ARF, p53, Ligases, Transcription, Factors, NSC652287, Tocris Bioscience, Ubiquitin E3 Ligase Inhibitors
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