RITA

Pricing Availability Delivery Time Qty
Cat.No. 2443 - RITA | C14H12O3S2 | CAS No. 213261-59-7
Description: MDM2-p53 interaction inhibitor
Alternative Names: NSC 652287
Chemical Name: 5,5'-(2,5-Furandiyl)bis-2-thiophenemethanol
Purity: ≥97% (HPLC)
Datasheet
Citations (1)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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:


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View all Ubiquitin E3 Ligase Inhibitors

Keywords: p53-MDM2 interaction inhibitors inhibits antitumor agent MDM2-p53 MDM2 p14ARF p53 Ligases Transcription Factors NSC652287 NSC 652287 Ubiquitin E3 Ligases

1 Citation for RITA

Citations are publications that use Tocris products. Selected citations for RITA include:

Thotala et al (2012) Glycogen synthase kinase 3β inhibitors protect hippocampal neurons from radiation-induced apoptosis by regulating MDM2-p53 pathway. Cell Death Differ 19 387 PMID: 21738215


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Literature in this Area

Programmed Cell Death

Programmed Cell Death Poster

There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.

Pathways for RITA

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