RITA
Reactivation of p53 and induction of tumor cell apoptosis (RITA) is an activator of p53 that exhibits anticancer chemotherapeutic and anti-angiogenic activities. In vivo, RITA downregulates expression of VEGF, HIF-1α, p21, and HDM2. In cellular and animal models of neuroblastoma, RITA inhibits expression of N-Myc, AurK, Mcl-1, Bcl-2, MDM2, and MDMX, inducing apoptosis and inhibiting growth. Similar effects are observed in models of gastrointestinal stromal tumors and cervical carcinoma.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18959810
| Cas No. |
213261-59-7 |
|---|---|
| Purity |
≥98% |
| Formula |
C14H12O3S2 |
| Formula Wt. |
292.37 |
| IUPAC Name |
[5-[5-[5-(hydroxymethyl)thiophen-2-yl]furan-2-yl]thiophen-2-yl]methanol |
| Synonym |
Reactivation of p53 and induction of tumor cell apoptosis |
Burmakin M, Shi Y, Hedström E, et al. Dual targeting of wild-type and mutant p53 by small molecule RITA results in the inhibition of N-Myc and key survival oncogenes and kills neuroblastoma cells in vivo and in vitro. Clin Cancer Res. 2013 Sep 15;19(18):5092-103. PMID: 23864164.
Henze J, Mühlenberg T, Simon S, et al. p53 modulation as a therapeutic strategy in gastrointestinal stromal tumors. PLoS One. 2012;7(5):e37776. PMID: 22662219.
Zhao CY, Szekely L, Bao W, et al. Rescue of p53 function by small-molecule RITA in cervical carcinoma by blocking E6-mediated degradation. Cancer Res. 2010 Apr 15;70(8):3372-81. PMID: 20395210.
Yang J, Ahmed A, Poon E, et al. Small-molecule activation of p53 blocks hypoxia-inducible factor 1alpha and vascular endothelial growth factor expression in vivo and leads to tumor cell apoptosis in normoxia and hypoxia. Mol Cell Biol. 2009 Apr;29(8):2243-53. PMID: 19223463.
