p53 Activator III, RITAA trycyclic thiophene derivative that binds MDM2, activates p53 and induces apoptosis

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

p53 Activator III, RITA | CAS 213261-59-7 is rated 5.0 out of 5 by 1.
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Synonym: 2,5-bis-(5-Hydroxymethyl-2-thienyl)-furan; NSC 652287
Application: 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
* Refer to Certificate of Analysis for lot specific data (including water content).
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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 RITA induces DNA damage, and DNA-DNA, DNA-protein crosslinks. Furthermore, low concentrations of 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 RITA has been reported to cause an increases of p53 protein levels, reduces p21(WAF1) protein levels, and induce apoptosis.


References

1. Rivera, M.I., et al. 1999. Biochem. Pharmacol. 57: 1283-1295. PMID: 10230772
2. Nieves-Neira, W., et al. 1999. Mol. Pharmacol. 56: 478-484. PMID: 10462535
3. Issaeva, N., et al. 2004. Nat. Med. 10: 1321-1328. PMID: 15558054

Physical State :
Solid
Solubility :
Soluble in DMSO (58 mg/ml at 25° C), ethanol (8 mg/ml at 25° C), DMF (30 mg/ml), 1:1 solution of dimethyl formamide: PBS (pH 7.2) (0.5 mg/ml, dissolve RITA first in dimethyl formamide and then dilute with PBS), and water (<1 mg/ml at 25° C).
Storage :
Store at -20° C
Melting Point :
205.30° C (Predicted)
Boiling Point :
~464.9° C at 760 mmHg (Predicted)
Density :
~1.40 g/cm3 (Predicted)
Refractive Index :
n20D 1.66 (Predicted)
IC50 :
A498 cells: IC50 = 2 nM; TK-10 cells: IC50 = 20 nM; ACHN: IC50 = 13 µM; UO-31: IC50 = 37 µM
pK Values :
pKa: 13.43 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
374536
MDL Number :
MFCD03235294
SMILES :
C1=C(SC(=C1)C2=CC=C(O2)C3=CC=C(S3)CO)CO

Download SDS (MSDS)

Certificate of Analysis

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p53 Activator III, RITA  Product Citations

See how others have used p53 Activator III, RITA. Click on the entry to view the PubMed entry .

Citations 1 to 6 of 6 total

PMID: # 30447254  Azatyan, A.|Gallo-Oller, G.|Diao, Y.|Selivanova, G.|Johnsen, JI.|Zaphiropoulos, PG.| et al. 2019. Cancer Lett. 442: 341-350.

PMID: # 28608259  Qiu, M. et al. 2017. Cancer Chemother. Pharmacol. 80: 275-286.

PMID: # 22166212  Ma, T. et al. 2012. Biochem. Biophys. Res. Commun. 417: 931-7.

PMID: # 15558054  Issaeva, N. et al. 2004. Nature Medicine. 10: 1321-1327.

PMID: # 10230772  Rivera, MI. et al. 1999. Biochem. Pharmacol. 57: 1283-1295.

PMID: # 10462535  Nieves-Neira, W. et al. 1999. Mol. Pharmacol. 56: 478-484.

Citations 1 to 6 of 6 total

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 Mcl A 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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