RITA

HDM-2 (human double minute-2, MDM-2 in mouse) is a key negative regulator of p53 that binds to and targets p53 for proteasomal degradation. Overexpression of HDM-2 in some tumors leads to inactivation of p53 thereby allowing tumor cells to escape p53-induced apoptosis. RITA is an inhibitor of the protein-protein interaction between p53 and human double minute-2 (HDM-2). 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). In vivo, RITA (10 mg/kg) reduces tumor volume in an HCT116 mouse xenograft model. It also induces complete tumor regression in an A498 mouse xenograft model when administered at a dose of 45 mg/kg.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: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:1): .5 mg/ml, DMSO: 20 mg/ml, Ethanol: 1 mg/ml. lambdamax: 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.