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RITA

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Chemical Structure| 213261-59-7 同义名 : NSC 652287;2,5-bis(5-hydroxymethyl-2-thienyl) Furan;Reactivation of p53 and Induction of Tumor Cell Apoptosis
CAS号 : 213261-59-7
货号 : A440096
分子式 : C14H12O3S2
纯度 : 99%+
分子量 : 292.373
MDL号 : MFCD03235294
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(359.13 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • E3 Ligase
描述 RITA (NSC 652287), a representative of a series of thiophene derivatives, is a DNA damage inducing agent that induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks and exhibits potent and selective antitumor activity against several tumor cell lines[3]. The renal carcinoma cell line A498 treated with 10 nM NSC 652287 exhibited cell cycle arrest in G(0)-G(1) and G(2)-M, with increased p53 and p21(WAF1) protein. NSC 652287 at higher concentrations still induced p53 elevation but with p21(WAF1) reduction and massive apoptosis[3]. MCF-7 and MDA-MB-231 cells were treated with RITA (1 μM) for 24 h in normoxia and hypoxia (1% O2) and there was a clear increase in rounding and displacement of cells from monolayers in tissue culture, indicative of apoptosis, to a similar extent in normoxia and hypoxia[4]. RITA exhibits potent antileukemic properties against p53-null chronic myeloid leukemia (CML)-derived K562 cells by triggering apoptosis through caspase-9 and caspase-3 activation and poly (ADP-ribose) polymerase cleavage, in a dose- and time-dependent manner (1,2 and 4 µM)[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.42mL

0.68mL

0.34mL

17.10mL

3.42mL

1.71mL

34.20mL

6.84mL

3.42mL
参考文献

[1]Roh JL, Ko JH, et al. The p53-reactivating small-molecule RITA enhances cisplatin-induced cytotoxicity and apoptosis in head and neck cancer. Cancer Lett. 2012 Dec 1;325(1):35-41.

[2]Rivera MI, Stinson SF, et al. Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines: differential accumulation and metabolism. Biochem Pharmacol. 1999 Jun 1;57(11):1283-95.

[3]Nieves-Neira W, Rivera MI, Kohlhagen G, Hursey ML, Pourquier P, Sausville EA, Pommier Y. 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. doi: 10.1124/mol.56.3.478. PMID: 10462535.

[4]Yang J, Ahmed A, Poon E, Perusinghe N, de Haven Brandon A, Box G, Valenti M, Eccles S, Rouschop K, Wouters B, Ashcroft M. 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. doi: 10.1128/MCB.00959-08. Epub 2009 Feb 17. PMID: 19223463; PMCID: PMC2663300.

[5]Mobaraki RN, Karimi M, Alikarami F, Farhadi E, Amini A, Bashash D, Paridar M, Kokhaei P, Rezvani MR, Kazemi A, Safa M. RITA induces apoptosis in p53-null K562 leukemia cells by inhibiting STAT5, Akt, and NF-κB signaling pathways. Anticancer Drugs. 2018 Oct;29(9):847-853. doi: 10.1097/CAD.0000000000000651. PMID: 30157040.