Date published: 2026-4-5

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p53 Activator III, RITA (CAS 213261-59-7)

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Alternate Names:
2,5-bis-(5-Hydroxymethyl-2-thienyl)-furan; NSC 652287
Application:
p53 Activator III, RITA is a trycyclic thiophene derivative that binds MDM2, activates p53 and induces apoptosis
CAS Number:
213261-59-7
Purity:
>97%
Molecular Weight:
292.37
Molecular Formula:
C14H12O3S2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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p53 Activator III, RITA, also referred to as NSC 652287, is a trycyclic thiophene derivative that binds to MDM2, disrupting the MDM2-p53 complex and subsequently activating p53 and inducing apoptosis. Renal carcinoma research has demonstrated that p53 Activator III, RITA induces DNA damage, and DNA-DNA, DNA-protein crosslinks. Furthermore, low concentrations of p53 Activator III, RITA caused cell cycle arrest in G0-G1 and G2-M, and elevated p53 and p21(WAF1) protein levels in renal carcinoma studies. At higher concentrations p53 Activator III, RITA has been reported to cause an increases of p53 protein levels, reduces p21(WAF1) protein levels, and induce apoptosis.

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

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p53 Activator III, RITA (CAS 213261-59-7) References

  1. Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines: differential accumulation and metabolism.  |  Rivera, MI., et al. 1999. Biochem Pharmacol. 57: 1283-95. PMID: 10230772
  2. DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells.  |  Nieves-Neira, W., et al. 1999. Mol Pharmacol. 56: 478-84. PMID: 10462535
  3. Identification of the major metabolite of 2,5-bis(5-hydroxymethyl-2-thienyl)furan (NSC 652287), an antitumor agent, in the S9 subcellular fraction of dog liver cells.  |  Phillip, LR., et al. 2002. J Chromatogr B Analyt Technol Biomed Life Sci. 767: 27-33. PMID: 11863292
  4. Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors.  |  Issaeva, N., et al. 2004. Nat Med. 10: 1321-8. PMID: 15558054
  5. p53-dependent inhibition of TrxR1 contributes to the tumor-specific induction of apoptosis by RITA.  |  Hedström, E., et al. 2009. Cell Cycle. 8: 3584-91. PMID: 19838062
  6. Inhibition of hypoxia-inducible factor-1alpha (HIF-1alpha) protein synthesis by DNA damage inducing agents.  |  Lou, JJ., et al. 2010. PLoS One. 5: e10522. PMID: 20479887
  7. Pharmacological activation of a novel p53-dependent S-phase checkpoint involving CHK-1.  |  Ahmed, A., et al. 2011. Cell Death Dis. 2: e160. PMID: 21593792
  8. Synthesis of heterocyclic triads by Pd-catalyzed cross-couplings and evaluation of their cell-specific toxicity profile.  |  Salamoun, J., et al. 2014. Org Lett. 16: 2034-7. PMID: 24641272
  9. Dual targeting of p53 and c-MYC selectively eliminates leukaemic stem cells.  |  Abraham, SA., et al. 2016. Nature. 534: 341-6. PMID: 27281222
  10. Specific RITA Modification Produces Hyperselective Cytotoxicity While Maintaining In Vivo Antitumor Efficacy.  |  Peyser, BD., et al. 2019. Mol Cancer Ther. 18: 1765-1774. PMID: 31341033
  11. Mdm2-P53 Interaction Inhibitor with Cisplatin Enhances Apoptosis in Colon and Prostate Cancer Cells In-Vitro.  |  Gupta, A., et al. 2019. Asian Pac J Cancer Prev. 20: 3341-3351. PMID: 31759358
  12. Direct conversion of human fibroblasts into dopaminergic neuron-like cells using small molecules and protein factors.  |  Qin, H., et al. 2020. Mil Med Res. 7: 52. PMID: 33129359
  13. Division of labor within the DNA damage tolerance system reveals non-epistatic and clinically actionable targets for precision cancer medicine.  |  Spanjaard, A., et al. 2022. Nucleic Acids Res. 50: 7420-7435. PMID: 35819193

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

p53 Activator III, RITA, 1 mg

sc-202753
1 mg
$112.00

p53 Activator III, RITA, 10 mg

sc-202753A
10 mg
$273.00

p53 Activator III, RITA, 100 mg

sc-202753B
100 mg
$1564.00

p53 Activator III, RITA, 500 mg

sc-202753C
500 mg
$5205.00

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. p53 Activator III, RITA, sc-202753, is in yellow powder form.
Answered by: Chemical Support 4
Date published: 2017-07-07
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Rated 5 out of 5 by from A decrease in MclA decrease in Mcl-1 protein expression observed by WB in HCT 116 cells post treatment with p53 Activator, RITA. An increase was observed in the same cell line by WB for p53 expression. -SCBT QC
Date published: 2015-03-07
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p53 Activator III, RITA is rated 5.0 out of 5 by 1.
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