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RITACat. No. 2443 |
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Alternative Name: NSC 652287 Chemical Name: 5,5'-(2,5-Furandiyl)bis-2-thiophenemethanol |
Biological Activity
Anti-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.Certificate of Analysis / Safety Data Sheet
References
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
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