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RITA
Cayman Chemical Item Number 10006426
Description
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.1↗ RITA (reactivation of p53 and induction of tumor cell apoptosis) is a small molecule inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53.2↗ It binds to p53 with an apparent Kd of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation and activation.2↗ RITA potently inhibits the growth of a variety of cancer cell lines in the sub-micromolar range, inducing both DNA-protein and DNA-DNA cross links in human renal cancer cells.3↗ RITA reduced tumor size by 90% at a dose of 10 mg/kg in SCID mice bearing HCT116 tumors, and caused complete regression of A-498 tumor cell xenografts in nude mice at a dose of 45 mg/kg.2↗,4↗
Synonyms 2,5-bis(5-hydroxymethyl-2-thienyl) Furan
NSC 652287
Formal Name 5,5'-(2,5-furandiyl)bis-2-thiophenemethanol
CAS Number 213261-59-7
Molecular Formula C14H12O3S2
Formula Weight 292.4
Formulation A crystalline solid
Purity >98%
λmax 265, 359 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES OCc1ccc(s1)c1ccc(o1)c1ccc(CO)s1
InCHI Code 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 |