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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.
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.
| Cell Experiment | |
|---|---|
| Cell lines | U2OS cells |
| Preparation 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). |
| Concentrations | 25 μM |
| Incubation time | 1 h |
| Animal Experiment | |
|---|---|
| Animal models | 069(nu)/070(nu/+) athymic nude mice |
| Formulation | 3:1 DMSO:PBS |
| Dosages | 3 mg/kg |
| Administration | i.p. |
| Molecular Weight | 459.95 |
| Formula | C22H22ClN3O4S |
| CAS Number | 1943733-16-1 |
| Solubility (25°C) | 91 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| ZL-2201
ZL-2201 is a potent DNA-PK inhibitor with an IC50 of 1 nM. |
| AMA-37
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| PIK-75
PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis. |
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