Inhibitor of p53/HDM2 interaction. Activator of p53 function in tumors. Potently inhibits the growth of a variety of cancer cell lines in the submicromolar range. It has been suggested that RITA selectively targets cells expressing p53 by other mechanisms than direct binding to the N-terminal domain of p53.
Product Details
| Alternative Name: | Reactivation of p53 and Induction of Tumor Cell Apoptosis, 2,5-bis(5-Hydroxymethyl-2-thienyl)furan, NSC652287 |
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| Formula: | C14H12O3S2 |
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| MW: | 292.4 |
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| CAS: | 213261-59-7 |
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| Purity: | ≥98% (HPLC) |
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| Appearance: | White to brown crystalline solid. |
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| Solubility: | Soluble in 100% ethanol (1mg/ml), DMSO (20mg/ml), dimethyl formamide (30mg/ml); 0.5mg/ml soluble in a 1:1 solution of dimethyl formamide: PBS (pH 7.2) (dissolve RITA first in dimethyl formamide and then dilute with PBS). |
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| Shipping: | Blue Ice |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stable for at least two years after receipt when stored at -20°C. We do not recommend storing aqueous solutions for more than one day. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
NMR indicates that the small molecule RITA does not block p53-MDM2 binding in vitro: M. Krajewski, et al.; Nat. Med.
11, 1135 (2005),
Abstract;
Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors: N. Issaeva, et al.; Nat. Med.
10, 1321 (2004),
Abstract;
DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells: W. Nieves-Neira, et al.; Mol. Pharmacol.
56, 478 (1999),
Abstract;
Full Text
Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines: differential accumulation and metabolism: M.I. Rivera, et al.; Biochem. Pharmacol.
57, 1283 (1999),
Abstract;
