All AbMole products are for research use only, cannot be used for human consumption.
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 |
| Related DNA-PK Products |
|---|
| NU7026
NU7026 is a DNA-PK inhibitor with IC50 of 0.23 μM. |
| KU-0060648
KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM. |
| CC-115
CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM). CC-115 inhibits PC-3 cells proliferation with an IC50 of 138 nM. CC-115 blocks both mTORC1 and mTORC2 signaling. |
| LTURM34
LTURM34 is a specific DNA-PK inhibitor, 170-fold more selective for DNA-PK activity compared to PI3K activity, with IC50 value of 0.034 μM. |
| Compound 401
Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM) that also targets mTOR but not PI3K in vitro. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
