SJB2-043

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Chemical Structure| 63388-44-3 同义名 : -
CAS号 : 63388-44-3
货号 : A434626
分子式 : C17H9NO3
纯度 : 99%+
分子量 : 275.258
MDL号 : MFCD26960957
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 3 mg/mL(10.9 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
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
1mg 5mg 10mg

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

[1]Mistry H, Hsieh G, et al. Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells. Mol Cancer Ther. 2013 Dec;12(12):2651-62.

[2]Mistry H, Hsieh G, Buhrlage SJ, Huang M, Park E, Cuny GD, Galinsky I, Stone RM, Gray NS, D'Andrea AD, Parmar K. Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells. Mol Cancer Ther. 2013 Dec;12(12):2651-62.