切换导航

RI-1

现货
Catalog No.
A3764
RAD51抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 830.00
现货
5mg
¥ 750.00
现货
10mg
¥ 1,300.00
现货
50mg
¥ 5,000.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

RI-1 Description:IC50: 5~30 μM [1]
RAD51 is a eukaryote gene, encoding RAD51 protein that participates in DNA damage induction and complex signal pathway of cell cycle checkpoint of homologous recombination in cells. RI-1 inhibits the over-expression of RAD51 in cancer cells by bonding covalently to the surface of RAD51 protein at Cys 319 and irreversibly loosen a protein-protein interface that is essential for filament formation and recombinase activity.
In vitro: RI-1 binds covalently to the surface of RAD51 protein at cysteine 319 that likely destabilizes an interface used by RAD51 monomers to oligomerize into filaments on DNA. Correspondingly, the molecule inhibits the formation of subnuclear RAD51 foci in cells following DNA damage, while leaving replication protein A focus formation unaffected. Finally, it potentiates the lethal effects of a DNA cross-linking drug in human cells. Given that this inhibitory activity is seen in multiple human tumor cell lines, RI-1 holds promise as an oncologic drug [1].
In vivo: There are limits to the development of RI-1 in pre-clinical in vivo models due to its short half-life in tissue culture media and aqueous buffers. RI-2, a homolog of RI-1, was created that mitigated these effects(119). RI-2 was shown to bind Rad51 and inhibit the nuclear foci of Rad51 at sites of DNA damage. RI-2 is currently the subject of further in vitro and in vivo studies and is being used to identify third generation analogs that inhibit the function of Rad51 [2].
Clinical trial: Up to now, RI-1 is still in the preclinical development stage.
Reference:
[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.

Chemical Properties

StorageStore at -20°C
M.Wt361.61
Cas No.415713-60-9
FormulaC14H11Cl3N2O3
Solubility≥18.1 mg/mL in DMSO, ≥8.89 mg/mL in EtOH with gentle warming, <2.18 mg/mL in H2O
Chemical Name3-chloro-1-(3,4-dichlorophenyl)-4-morpholin-4-ylpyrrole-2,5-dione
SDFDownload SDF
Canonical SMILESC1COCCN1C2=C(C(=O)N(C2=O)C3=CC(=C(C=C3)Cl)Cl)Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

生物活性

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

化学结构

RI-1