An inhibitor of the p53-HDM-2 interaction
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RITA

Item No. 10006426

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5,5'-(2,5-furandiyl)bis-2-thiophenemethanol
CAS Number
213261-59-7
Synonyms
  • 2,5-bis(5-hydroxymethyl-2-thienyl) Furan
  • NSC 652287
  • Reactivation of p53 and Induction of Tumor Cell Apoptosis
Molecular Formula
C14H12O3S2
Formula Weight
292.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): .5 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/ml
λmax
265, 359 nm
SMILES
OCc1ccc(s1)c1ccc(o1)c1ccc(CO)s1
InChi Code
InChI=1S/C14H12O3S2/c15-7-9-1-5-13(18-9)11-3-4-12(17-11)14-6-2-10(8-16)19-14/h1-6,15-16H,7-8H2
InChi Key
KZENBFUSKMWCJF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $71

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    5 mg

    $146

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    10 mg

    $228

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    50 mg

    $1,056

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    Cayman Chemical
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    Product Description

    RITA is an inhibitor of the protein-protein interaction between p53 and human double minute-2 (HDM-2).1 It binds to p53 with an apparent Kd value of 1.5 nM and prevents the interaction between p53 and HDM-2. RITA induces DNA damage and apoptosis in, as well as inhibits the growth of, A498, TK-10, ACHN, and UO-31 renal carcinoma cells (GI50s = 0.017, 0.032, 22.76, and 41.71 µM, respectively).2 In vivo, RITA (10 mg/kg) reduces tumor volume in an HCT116 mouse xenograft model.1 It also induces complete tumor regression in an A498 mouse xenograft model when administered at a dose of 45 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Issaeva, N., Bozko, P., Enge, M., et al. Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activities p53 function in tumors. Nat. Med. 10(12), 1321-1328 (2004).

    2. Rivera, M.I., Stinson, S.F., Vistica, D.T., et al. Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines. Differential accumulation and metabolism. Biochem. Pharmacol. 57(11), 1283-1295 (1999).