RI-1
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
描述:IC50值为5~30 μM[1].
RAD51是一种真核生物基因,编码RAD51蛋白,在细胞中该蛋白参与DNA损伤诱导和同源重组细胞周期检验点的复杂信号通路.RI-1与位于RAD51蛋白表面的319位半胱氨酸共价结合,以抑制癌细胞中RAD51的过表达,且不可逆地疏松纤维形成和重组酶活性所必需的蛋白-蛋白相互作用界面.
体外实验:RI-1与位于RAD51蛋白表面的319位半胱氨酸共价结合,,其可能使DNA上用于将RAD51单体寡聚化成纤维的界面失稳.相应地,DNA损伤后,该分子抑制细胞中亚核RAD51灶的形成,但不影响复制蛋白A灶的形成.最后,其在人类细胞中加强DNA交联药物的致死效应.由于在多种人肿瘤细胞系中具有抑制活性,故RI-1是一种有前景的肿瘤药物[1].
体内实验:由于RI-1在组织培养基和水缓冲液中的半衰期短,RI-1在临床前体内模型中的发展有限.作为RI-1的同系物,RI-2的研制可缓解此类效应(119).RI-2可结合Rad51,且抑制DNA损伤处的Rad51核灶.目前RI-2是体内外进一步研究的对象,是用于鉴定可抑制Rad51功能的第三代类似物[2].
临床试验:到目前为止,RI-1仍处于临床前发展阶段.
参考文献：
[1] Budke B, Logan HL, Kalin JH, Zelivianskaia AS, Cameron McGuire W, Miller LL, Stark JM, Kozikowski AP, Bishop DK, Connell PP. RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells. Nucleic Acids Res. 2012;40(15):7347-57.
[2] Christian Jekimovs, Emma Bolderson, Amila Suraweera, Mark Adams, Kenneth J. O’Byrne, and Derek J. Richard. Chemotherapeutic Compounds Targeting the DNA Double-Strand Break Repair Pathways: The Good, the Bad, and the Promising. Front Oncol. 2014; 4: 86.
| Storage | Store at -20°C |
| M.Wt | 361.61 |
| Cas No. | 415713-60-9 |
| Formula | C14H11Cl3N2O3 |
| Solubility | insoluble in H2O; ≥18.1 mg/mL in DMSO; ≥8.89 mg/mL in EtOH with gentle warming |
| Chemical Name | 3-chloro-1-(3,4-dichlorophenyl)-4-morpholin-4-ylpyrrole-2,5-dione |
| SDF | Download SDF |
| Canonical SMILES | C1COCCN1C2=C(C(=O)N(C2=O)C3=CC(=C(C=C3)Cl)Cl)Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | RI-1是一种细胞可透过性的RAD51抑制剂. | |||||
| 靶点 | RAD51 | |||||
| IC50 | 5~30 μM | |||||
质量控制和MSDS
- 批次:
化学结构
