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My CartCAS：213261-59-7
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 213261-59-7 |
| Name | RITA |
| Molecular Formula | C14H12O3S2 |
| Molecular Weight | 292.37 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 200-256-5 |
| MDL | MFCD03235294 |
| SMILES | OCC1=CC=C(C2=CC=C(C3=CC=C(CO)S3)O2)S1 |
| Target Point | p53 |
| Passage | Apoptosis |
| Background | RITA is a potent inhibitor of the p53-HDM-2 interaction. |
| Biological Activity | RITA 是一种有效的 p53-HDM-2 相互作用抑制剂，可与 p53dN 结合，Kd 值为 1.5 nM，同时能够诱导 DNA-DNA 交联。[1-3] |
| In Vitro | RITA抑制p53-HDM-2相互作用，与p53dN结合，Kd为1.5 nM。 RITA(10μM)阻断HCT116细胞和HDF以及NHF-ERMyc细胞中p53和HDM-2之间的复合物形成，而与c-Myc表达无关。 RITA(0.5μM)以野生型p53依赖性方式降低肿瘤细胞的活力。此外，RITA(0.1μM)诱导p53依赖性细胞凋亡。 RITA诱导p53但不通过DNA损伤信号通路[1]。 RITA(NSC 652287)诱导DNA-DNA交联。 RITA诱导10nM的G2-M细胞周期停滞并导致100nM的细胞凋亡。 RITA(100 nM)也会升高p53并对p21WAF1蛋白水平产生剂量依赖性影响[2]。 RITA抑制HeLa和CaSki细胞的生长，IC50为1和10μM。此外，RITA(1μM)通过抑制p53/E6AP相互作用来稳定p53 [3]。 |
| In Vivo | RITA(0.1，1或10 mg/kg，ip)在携带HCT116和HCT116 TP53 - / - 异种移植物的SCID小鼠中显示出有效的抗肿瘤活性[1]。 RITA(10 mg/kg，ip)也抑制SCID小鼠中HeLa细胞的生长[3]。 |
| Cell Experiment | 对于细胞活力测定，将每孔3，000个细胞接种在96孔板中并用RITA处理48小时，之后用增殖试剂WST-1评估细胞活力。对于集落形成测定，将细胞接种在12孔板中并用RITA处理24小时，之后更换培养基并使细胞生长10-14天。菌落用结晶紫染色。对于生长曲线，将3000个细胞/ mL接种在12孔板中，用RITA处理，并在5天内计数[3]。 |
| Animal Experiment | 小鼠[1]使用在90％基质胶中的1×10 6个细胞，将4-6周龄的雌性SCID小鼠植入皮下异种移植物。在注射细胞后3-6天建立可触知的肿瘤，此时开始RITA治疗。通过静脉内或腹膜内注射在总体积为100μL的磷酸盐缓冲盐水中每天施用0.1，1或10mg/kg的RITA[1]。 |
| Data Literature Source | [1]. Issaeva N，et al. Small molecule RITA binds to p53，blocks p53-HDM-2 interaction and activates p53 function in tumors. Nat Med. 2004 Dec;10(12):1321-8. Epub 2004 Nov 21. [2]. Nieves-Neira W，et al. DNA protein cross-links produced by NSC 652287，a novel thiophene derivative active against human renal cancer cells. Mol Pharmacol. 1999 Sep;56(3):478-84. [3]. Zhao CY，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. |
| Unit | Bottle |
| Specification | 5mg 10mg 50mg |
RITA 是一种有效的 p53-HDM-2 相互作用抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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