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DNA Damage/DNA Repair DNA-PK YU238259

YU238259

Catalog No. T4339   CAS 1943733-16-1

YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays.

YU238259, CAS 1943733-16-1
Pack Size Availability Price/USD Quantity
2 mg In stock 65.00
5 mg In stock 107.00
10 mg In stock 185.00
25 mg In stock 380.00
50 mg In stock 673.00
100 mg In stock 1100.00
1 mL * 10 mM (in DMSO) In stock 118.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays.
Targets&IC50 HDR,  
In vitro YU238259 sensitizes tumor cells to radiation therapy and DSB-inducing chemotherapy. Treatment with YU238259 is not only synergistic with ionizing radiation (IR), etoposide, and PARP inhibition, but this synergism is heightened by BRCA2-deficiency. Synthetic lethality of YU238259 in HDR-deficient cells results from accumulation of unresolved DSBs following additional inhibition of residual HDR pathway activity. Inhibition of HDR activity by YU238259 has little to no effect on the NHEJ pathway.
In vivo Growth of BRCA2-deficient human tumor xenografts in nude mice is significantly delayed by YU238259 treatment even without concomitant DNA-damaging therapy.
Animal Research
Animal Models: 069(nu)/070(nu/+) athymic nude mice. Formulation: 3:1 DMSO:PBS. Dosages: 3 mg/kg . Administration: i.p
Animal Model:
Cell Research
U2OS cells were pretreated with 25 μM YU238259 or DMSO vehicle for 1 h and cells were then irradiated with 10 Gy IR. Cells were fixed at 8 h post-IR, stained with antibodies and Hoechst dye, and imaged. Foci were quantified using the InCell Analyzer algorithm developed by YCMD. Cells were scored as foci-positive if they contained ≥15 foci (BRCA1, pDNA-PK) or ≥20 foci (53BP1).
Molecular Weight 459.95
Formula C22H22ClN3O4S
CAS No. 1943733-16-1

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

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 )

Citations

References and Literature
1. Stachelek GC,etal.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.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Anti-cancer Compound Library

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