化合物YU238259 T4339

Product Introduction
Bioactivity


英文名: YU238259

描述: YU238259 是一种新型的同源依赖性 DNA 修复 (HDR) 抑制剂，在基于细胞的 GFP 报告基因检测中不抑制非同源末端连接 (NHEJ)，可研究癌症。

细胞实验: 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).

激酶实验: The cloning, expression and purification of USP21 from BL21 (DE3) bacteria are performed using standard molecular biology techniques. USP2, USP5, USP7, USP8, USP28, USP47, Ub-PLA2 (Ub-CHOP) and Ub-EKL (Ub-CHOP2) are generated. Caspase 3 and the caspase 3 substrate DEVD-Rh110 are used. Deubiquitylating enzyme, cathepsin B and 20S proteasome chymotrypsin like protease activities are measured. Caspase 3 activity is determined using a similar protocol. Briefly, dose ranges of compound (including USP7/USP47 inhibitor) are incubated with caspase 3 for 30 minutes before the addition of DEVD-Rh110 and reading on a fluorometric plate reader using excitation and emission maxima of 485 nm and 531 nm respectively. The final concentrations of caspase 3 and DEVD-Rh110 are 2 nM and 100 nM respectively

动物实验: Animal Models: 069(nu)/070(nu/+) athymic nude mice. Formulation: 3:1 DMSO:PBS. Dosages: 3 mg/kg . Administration: i.p

体外活性: 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.

体内活性: 在裸鼠体内，YU238259处理可延缓了BRCA2缺陷型人类肿瘤异种移植物的生长。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 84 mg/mL (182.6 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: inhibit | Inhibitor | YU 238259 | DNA-dependent protein kinase | DNA-PK | YU238259 | YU-238259

相关产品: PIK-75 | SF2523 | PI-3065 | PIK-75 hydrochloride | Torin 2 | KU-55933 | VX-984 | Compound 401 | Voxtalisib | Torin 1

相关库: Antioxidant Compound Library | Anti-Prostate Cancer Compound Library | Anti-Liver Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Neuronal Differentiation Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Glycolysis Compound Library

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