415713-60-9 Usage
Uses
Used in Anticancer Applications:
RI-1 is used as a chemical inhibitor for disrupting homologous recombination in human cells, which can enhance the killing of tumor cells by DNA-damaging agents. It is particularly effective in potentiating the killing of glioblastoma cells by ionizing radiation and alkylating drugs.
Used in Research:
RI-1 is used as a novel tool for studying DNA repair mechanisms in cells, providing valuable insights into the role of RAD51 in homologous recombination and its potential as a therapeutic target for cancer treatment.
Used in Drug Development:
RI-1 is used in the development of new cancer therapies that target RAD51 and homologous recombination, potentially leading to more effective treatments for various types of cancer.
Biochem/physiol Actions
RI-1 is a cell-permeable RAD51 inhibitor that binds covalently to the protein surface at Cysteine 319. RI-1 disrupts homologous recombination in human cells.
References
1) Anand et al. (2017), Rad51-mediated double-strand break repair and mismatch correction of divergent substrates; Nature, 544 377
2) Budke et al. (2012), RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells; Nucleic Acids Res., 40 7347
3) Balbous et al. (2016), A radiosensitizing effect of RAD51 inhibition in glioblastoma stem-like cells; BMC Cancer, 16 604
4) Berte et al. (2016), Targeting Homologous Recombination by Pharmacological Inhibitors Enhances the Killing response of Glioblastoma Cells Treated with Alkylating Drugs; Mol. Cancer Ther., 15 2665
Check Digit Verification of cas no
The CAS Registry Mumber 415713-60-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,1,5,7,1 and 3 respectively; the second part has 2 digits, 6 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 415713-60:
(8*4)+(7*1)+(6*5)+(5*7)+(4*1)+(3*3)+(2*6)+(1*0)=129
129 % 10 = 9
So 415713-60-9 is a valid CAS Registry Number.
415713-60-9Relevant academic research and scientific papers
Inhibition of Bfl-1 with N-aryl maleimides
Cashman, John R.,MacDonald, Mary,Ghirmai, Senait,Okolotowicz, Karl J.,Sergienko, Eduard,Brown, Brock,Garcia, Xochella,Zhai, Dayong,Dahl, Russell,Reed, John C.
supporting information; experimental part, p. 6560 - 6564 (2010/12/24)
High-throughput screening of 66,000 compounds using competitive binding of peptides comprising the BH3 domain to anti-apoptotic Bfl-1 led to the identification of 14 validated 'hits' as inhibitors of Bfl-1. N-Aryl maleimide 1 was among the validated 'hits'. A chemical library encompassing over 280 analogs of 1 was prepared following a two-step synthesis. Structure-activity studies for inhibition of Bfl-1 by analogs of N-aryl maleimide 1 revealed a preference for electron-withdrawing substituents in the N-aryl ring and hydrophilic amines appended to the maleimide core. Inhibitors of Bfl-1 are potential development candidates for anti-cancer therapeutics.
