WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407907
Description: YU238259 Is a Novel Inhibitor of Homology-Dependent DNA Repair. YU238259 exhibits potent synthetic lethality in the setting of DNA damage response and DNA repair defects. YU238259 specifically inhibits homology-dependent DNA repair, but not non-homologous end-joining, in cell-based GFP reporter assays. Treatment with YU238259 is not only synergistic with ionizing radiation, etoposide, and PARP inhibition, but this synergism is heightened by BRCA2 deficiency.
MedKoo Cat#: 407907
Chemical Formula: C22H22ClN3O4S
Exact Mass: 459.102
Molecular Weight: 459.945
Elemental Analysis: C, 57.45; H, 4.82; Cl, 7.71; N, 9.14; O, 13.91; S, 6.97
Synonym: YU238259; YU-238259; YU 238259;
IUPAC/Chemical Name: N-(2-(5-chloropyridin-2-yl)ethyl)-4-(((4-methoxyphenyl)sulfonamido)methyl)benzamide
InChi Key: BIHURSOREGLQBB-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H22ClN3O4S/c1-30-20-8-10-21(11-9-20)31(28,29)26-14-16-2-4-17(5-3-16)22(27)24-13-12-19-7-6-18(23)15-25-19/h2-11,15,26H,12-14H2,1H3,(H,24,27)
SMILES Code: C1=CC(OC)=CC=C1S(=O)(=O)NCC1=CC=C(C(=O)NCCC2=CC=C(Cl)C=N2)C=C1
Further, growth of BRCA2-deficient human tumor xenografts in nude mice is significantly delayed by YU238259 treatment even in the absence of concomitant DNA-damaging therapy. The cytotoxicity of these small molecules in repair-deficient cells results from an accumulation of unresolved DNA double-strand breaks. YU238259 or related small molecules may have clinical benefit to patients with advanced BRCA2-negative tumors, either as a monotherapy or as an adjuvant to radiotherapy and certain chemotherapies.
1: Stachelek GC, Peterson-Roth E, Liu Y, Fernandez RJ 3rd, Pike LR, Qian JM,
Abriola L, Hoyer D, Hungerford W, Merkel J, Glazer PM. YU238259 Is a Novel
Inhibitor of Homology-Dependent DNA Repair That Exhibits Synthetic Lethality and
Radiosensitization in Repair-Deficient Tumors. Mol Cancer Res. 2015
Oct;13(10):1389-97. doi: 10.1158/1541-7786.MCR-15-0036. Epub 2015 Jun 26. PubMed
PMID: 26116172; PubMed Central PMCID: PMC4618103.