YU 238259

SKU: orb1225796

Description

YU 238259 is a novel DNA double-strand break repair inhibitor that exhibits potent synthetic lethality in the setting of DNA damage response and DNA repair defects; specifically inhibits homology-dependent DNA repair (HDR), but not non-homologous end-joining (NHEJ), in cell-based GFP reporter assays; significantly delays tumor growth of BRCA2-deficient human tumor xenografts in nude mice.

Key Properties

• CAS Number: 1943733-16-1
• MW: 459.95
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₂ClN₃O₄S
• SMILES: C1=CC(OC)=CC=C1S(=O)(=O)NCC1=CC=C(C(=O)NCCC2=CC=C(Cl)C=N2)C=C1
• Target: DNA Repair Protein
• Solubility: DMSO: 84 mg/mL (182.6 mM); Ethanol: <1 mg/mL; Water: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  YU238259 (3 mg/kg, i.p.) inhibits the growth of BRCA2-deficient tumor xenografts in nude mice.
• In Vitro:
  YU238259 is an inhibitor of homology-dependent DNA repair, with no effect on PARP activity. YU238259 shows cytotoxicity in BRCA2-deficient cells, with a low LD50 of 8.5 μM. YU238259 (0-5 μM) causes a potent, dose-dependent decrease in HDR efficiency in U2OS DR-GFP or U2OS EJ5-GFP cells, but with no effect on NHEJ frequency. YU238259 (0-10 μM) exhibits synthetic lethality with loss of frequently mutated tumor suppressors, and shows synergism with radiotherapy (IR) and DNA-damaging chemotherapy that is potentiated by BRCA2 loss.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

YU238259

Quick Database Links

Gene Symbol

DNA Repair Protein