Home DNA Damage/DNA Repair DNA-PK inhibitor YU238259 For research use only.

YU238259

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 Chemical Structure

YU238259 Chemical Structure

CAS No. 1943733-16-1

Purity & Quality Control

YU238259 Related Products

Signaling Pathway

DNA-PK Signaling Pathways

DNA-PK Signaling Pathway

Biological Activity

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
HDR [1]
In vitro
In vitro YU238259 exhibits potent synthetic lethality in the setting of DNA damage response and DNA repair defects. 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. YU238259 sensitizes tumor cells to radiation therapy and DSB-inducing chemotherapy [1].
Cell Research Cell lines U2OS cells
Concentrations 25 μM
Incubation Time 1 h
Method

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).
In Vivo
In vivo 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[1].
Animal Research Animal Models 069(nu)/070(nu/+) athymic nude mice
Dosages 3 mg/kg 
Administration i.p

Chemical Information & Solubility

Molecular Weight 459.95 Formula

C22H22ClN3O4S
CAS No. 1943733-16-1 SDF --
Smiles COC1=CC=C(C=C1)S(=O)(=O)NCC2=CC=C(C=C2)C(=O)NCCC3=NC=C(C=C3)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 91 mg/mL ( (197.84 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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