| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| N409189-1ml |
1ml |
现货  |
|
| 英文别名 | 4H-1-Benzopyran-4-one, 8-(4-dibenzothienyl)-2-(4-morpholinyl)- |
|---|---|
| 规格或纯度 | Moligand™, 2mM in DMSO |
| 英文名称 | NU7441 (KU-57788) |
| 生化机理 | NU7441（KU-57788）是一种强效的选择性 DNA-PK 抑制剂，IC50 为 14 nM，在无细胞实验中还能抑制 mTOR 和 PI3K，IC50 分别为 1.7 μM 和 5 μM。它能降低 NHEJ 的频率，同时提高 Cas9 介导的 DNA 切割后的 HDR 速率。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 蛋白激酶抑制剂；DNA 激活；催化亚基 |
| 产品介绍 |
KU-57788(NU7441)是DNA-PK选择性抑制剂，IC50为14 nM，对mTOR，PI3K，ATM和ATR的抑制性较弱。A DNA-PK inhibitor, and antitumor agent in vitro. Information NU7441 (KU-57788) NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing th NU7441 increases the persistence of γH2AX foci after ionizing radiation–induced or etoposide-induced DNA damage. NU7441 (0.5 μM or 1 μM) appreciably increases G2-M accumulation induced by ionizing radiation, etoposide, and doxorubicin in both SW620 and LoVo cells. NU7441 causes persistence of doxorubicin- and ionising radiation-induced DNA double-strand break and also slightly decreases homologous recombination activity DNA-PK-proficient M059-Fus-1 and DNA-PK-deficient M059 J human tumour cells. NU7441 inhibits UV-induced RPA p34 hyperphosphorylation in a dose-dependent manner both in cells lacking and cells expressing polymerase η. NU7441 increases levels of fludarabine-induced γH2AX foci and correspondingly decreased fludarabine-induced cell death in chronic lymphocytic leukemia cells. NU7441 also inhibits mitoxantrone-induced DNA-PKcs autophosphorylation and repair in chronic lymphocytic leukemia cells. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage. In vivo NU7441 intraperitoneally administrated at dose of 10 mg/kg maintains for at least 4 hours shows nontoxic and increases etoposide-induced tumor growth delay 2-fold in mice bearing SW620 xenografts. cell lines： Concentrations：0.5 μM or 1 μM Incubation Time：17 hours Powder Purity:≥99% |
| ALogP | 5.403 |
|---|---|
| hba_count | 3 |
| Rotatable Bond | 2 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | O=C1C=C(OC2=C1C=CC=C2C3=CC=CC4=C3SC5=C4C=CC=C5)N6CCOCC6 |
| 分子量 | 413.49 |
| Reaxy-Rn | 9876245 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=9876245&ln= |
| DMSO(mg / mL) Max Solubility | 4 |
|---|---|
| DMSO(mM) Max Solubility | 9.67 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 9876245 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=9876245&ln= |
| Concentration | 1-3（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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