Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 346 | 现货 | ||
2 mg | ¥ 498 | 现货 | ||
5 mg | ¥ 897 | 现货 | ||
10 mg | ¥ 1,580 | 现货 | ||
25 mg | ¥ 3,230 | 现货 | ||
50 mg | ¥ 4,790 | 现货 | ||
100 mg | ¥ 6,850 | 现货 | ||
500 mg | ¥ 13,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 898 | 现货 |
产品描述 | 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. |
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 | Growth of BRCA2-deficient human tumor xenografts in nude mice is significantly delayed by YU238259 treatment even without concomitant DNA-damaging therapy. |
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 |
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). |
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 |
分子量 | 459.95 |
分子式 | C22H22ClN3O4S |
CAS No. | 1943733-16-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 84 mg/mL (182.6 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1741 mL | 10.8707 mL | 21.7415 mL | 54.3537 mL |
5 mM | 0.4348 mL | 2.1741 mL | 4.3483 mL | 10.8707 mL | |
10 mM | 0.2174 mL | 1.0871 mL | 2.1741 mL | 5.4354 mL | |
20 mM | 0.1087 mL | 0.5435 mL | 1.0871 mL | 2.7177 mL | |
50 mM | 0.0435 mL | 0.2174 mL | 0.4348 mL | 1.0871 mL | |
100 mM | 0.0217 mL | 0.1087 mL | 0.2174 mL | 0.5435 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
YU238259 1943733-16-1 DNA Damage/DNA Repair Others PI3K/Akt/mTOR signaling DNA-PK inhibit Inhibitor YU 238259 DNA-dependent protein kinase YU-238259 inhibitor