| 产品描述: | DB2313 是一种有效的转录因子 PU.1 抑制剂,apoptosis 为 14 nM。DB2313 破坏了 PU.1 与靶基因启动子的相互作用。DB2313 可诱导急性髓细胞性白血病 (AML) 细胞凋亡 (apoptosis),并具有抗癌作用。 |
| 靶点: |
IC50: 14 nM (PU.1) |
| 体外研究: |
DB2313 treatment leads to a profound decrease in the growth of PU.1 URE–/– acute myeloid leukemia (AML) cells (IC50 of 7.1 μM), while showing little effect on normal hematopoietic cells at similar concentrations. DB2313 treatment leads to a 3.5-fold increase in apoptotic cells in murine PU.1 URE–/– AML cells. DB2313 also leads to a significant decrease in clonogenicity in the second and third rounds of plating and a complete disruption of clonogenic capacity in the fourth and higher rounds of plating. In AML cells, DB2313 decreases PU.1 occupancy on E2f1, Junb, and Csf1r promoters. |
| 体内研究: |
DB2313 (17 mg/kg; i.p.; three times per week; for 3 weeks) treatment decreases leukemia progression and results in increased survival in mice. |
| 参考文献: |
1. Iléana Antony-Debré, et al. Pharmacological inhibition of the transcription factor PU.1 in leukemia. J Clin Invest. 2017 Dec 1;127(12):4297-4313.
2. Zhang S, Zhao S, Qi Y, et al. SPI1-induced downregulation of FTO promotes GBM progression by regulating pri-miR-10a processing in an m6A-dependent manner. Mol Ther Nucleic Acids. 2022;27:699-717. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.411 ml |
7.054 ml |
14.108 ml |
| 5 mM |
0.282 ml |
1.411 ml |
2.822 ml |
| 10 mM |
0.141 ml |
0.705 ml |
1.411 ml |
| 50 mM |
0.028 ml |
0.141 ml |
0.282 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |