| 应用 |
A trycyclic thiophene derivative that binds MDM2, activates p53 and induces apoptosis. |
| 产品介绍 |
RITA (NSC 652287)诱导DNA-蛋白质和DNA-DNA交联，检测不到DNA单链断裂，通过靶向作用于p53，也抑制MDM2-p53相互作用。 |
| 备注 |
RITA (NSC 652287) induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and also inhibits MDM2-p53 interaction by targeting p53. |
| 生化机理 |
p53 Activator III, RITA, also referred to as NSC 652287, is a trycyclic thiophene derivative that binds to MDM2, disrupting the MDM2-p53 complex and subsequently activating p53 and inducing apoptosis. Renal carcinoma research has demonstrated that RITA induces DNA damage, and DNA-DNA, DNA-protein crosslinks. Furthermore, low concentrations of RITA caused cell cycle arrest in G0-G1 and G2-M, and elevated p53 and p21(WAF1) protein levels in renal carcinoma studies. At higher concentrations RITA has been reported to cause an increases of p53 protein levels, reduces p21(WAF1) protein levels, and induce apoptosis. |
| 别名 |
SOS BISMETHANOL;2-Thiophenemethanol, 5,5'-(2,5-furandiyl)bis-;NSC 652287;NSC-652287;NSC652287;5,5'-(2,5-Furandiyl)bis-2-thiophenemethanol |
