SJB2-043
产品说明书
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同义名 : | - |
| CAS号 : | 63388-44-3 | |
| 货号 : | A434626 | |
| 分子式 : | C17H9NO3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 275.26 | |
| MDL号 : | MFCD26960957 | |
| 存储条件： |
Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | The ubiquitin-specific peptidases (USPs) are the main members of the deubiquitinase (DUB) family. USP1 by itself exhibits low DUB activity; however, this activity is significantly enhanced when bound as a USP1/UAF1 complex. SJB2-043 is an inhibitor of USP1/UAF1 with IC50 value of 0.544 μM. SJB2-043 inhibits the salvaging of DNA-binding-1 (ID1), FANC1 and FANCD2 proteins by Usp1 from proteosomal degradation and as a result caused an increase in cell death and sensitisation to DNA damaging agents. In vitro, SJB2-043 caused a dose-dependent decrease in the number of viable K562 cells, with an EC50 of approximately 1.07 μΜ. SJB2-043 induced apoptosis of chronic myelogenous leukemia (CML) K562 cells in a dose-dependent manner. In addition, low dose treatments with SJB2-043 activated differentiation of K562 cells into hemoglobin expressing erythroid cells. SJB2-043 exhibited dose-dependent cytotoxicity on the primary bone marrow as well as peripheral blood from AML patients. Moreover, SJB2-043 treatment caused inactivation of USP1 and promoted ID 1 degradation in primary AML cells[2]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.63mL 0.73mL 0.36mL |
18.16mL 3.63mL 1.82mL |
36.33mL 7.27mL 3.63mL |
| 参考文献 |
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