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RITA

Cat. No. M2578

All AbMole products are for research use only, cannot be used for human consumption.

RITA Structure
Synonym:

NSC 652287

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 37  USD37 In stock
5mg USD 65  USD65 In stock
10mg USD 110  USD110 In stock
50mg USD 360  USD360 In stock
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Quality Control & Documentation
Biological Activity

RITA (NSC 652287) induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and also inhibits MDM2-p53 interaction by targeting p53. RITA binds full-length p53 but not glutathione S-transferase (GST) protein or HDM-2. RITA blocks p53−HDM-2 interaction and p53 ubiquitination. RITA substantially decreases the amount of HDM-2 that coprecipitated with p53, although both proteins were upregulated. RITA induces activation of p53 in conjunction with up-regulation of phosphorylated ASK-1, MKK-4 and c-Jun. RITA also induces the activation of JNK signaling. RITA is well tolerated in mice after intraperitoneal administration, with no observable weight loss at doses up to 10 mg/kg during 1 month. After five injections of 0.1 mg/kg of RITA, the growth of the HCT116 tumors is suppressed by 40%, without apparent effects on the HCT116 TP53-/- tumors. At a dose of 1 or 10 mg/kg, RITA shows strong antitumor activity. HCT116 tumors are 90% smaller in mice treated with 10 mg/kg of RITA than in control untreated mice. RITA inhibits the tumor growth in a wild-type p53−dependent manner.

Product Citations
Customer Product Validations & Biological Datas
Source Oncotarget (2017). Figure 1. RITA
Method FACS analysis
Cell Lines HD-MB03 and DAOY cell
Concentrations 1 μM
Incubation Time 48 h
Results RITA treatment raised the apoptotic fraction in ONS-76 (P = 0.01) and DAOY (P = 0.03) cultures by 5-fold compared to controls, but had no significant effect on UW-228-2 apoptosis
Chemical Information
Molecular Weight 292.37
Formula C14H12O3S2
CAS Number 213261-59-7
Solubility (25°C) DMSO 48 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Carolyn Ying Zhao, et al. Cancer Res. Rescue of p53 function by small-molecule RITA in cervical carcinoma by blocking E6-mediated degradation

[2] Natalia Issaeva, et al. Nat Med. Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors

[3] W Nieves-Neira, et al. Mol Pharmacol. DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells

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Keywords: RITA, NSC 652287 supplier, p53, inhibitors, activators

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