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.
Technical Data
| M. Wt | 292.37 |
| Formula | C14H12O3S2 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 213261-59-7 |
| PubChem ID | 374536 |
| InChI Key | KZENBFUSKMWCJF-UHFFFAOYSA-N |
| Smiles | OCC1=CC=C(S1)C1=CC=C(O1)C1=CC=C(CO)S1 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 29.23 | 100 | |
| ethanol | 7.31 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 292.37. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.42 mL | 17.1 mL | 34.2 mL |
| 5 mM | 0.68 mL | 3.42 mL | 6.84 mL |
| 10 mM | 0.34 mL | 1.71 mL | 3.42 mL |
| 50 mM | 0.07 mL | 0.34 mL | 0.68 mL |
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References
References are publications that support the products' biological activity.
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
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
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 PMID:
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 PMID:
Keywords: RITA, supplier, p53-MDM2, interaction, inhibitors, inhibits, antitumor, agent, MDM2-p53, MDM2, p14ARF, p53, Ligases, Transcription, Factors, NSC652287, NSC, 652287, p53, Ubiquitin, E3, Ligases, Ubiquitin, E3, Ligases, Tocris Bioscience
