| 产品描述: | AZ-PFKFB3-67 is a potent and selective PFKFB3 kinase inhibitor with IC50s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1, respectively. AZ-PFKFB3-67 reduces MCL-1. AZ-PFKFB3-67 has neuroprotective activity[1][2][3]. |
| 体内研究: |
AZ-PFKFB3-67 (25 μM;) 可抑制细胞中的 PFKFB3 活性,表现为 SU-DHL-4 和 OCI-LY-1 细胞中MCL-1 蛋白水平的降低[2]。 AZ-PFKFB3-67 (10 nM; 24 h) 与 Roxadustat 联合处理可显著逆转氧糖剥夺条件下经Roxadustat 处理的神经元细胞死亡的增加[3]。 |
| 参考文献: |
1. Boyd S, et al. Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3. J Med Chem. 2015;58(8):3611-3625. 2. Sneyers F, et al. Intracellular BAPTA directly inhibits PFKFB3, thereby impeding mTORC1-driven Mcl-1 translation and killing MCL-1-addicted cancer cells. Cell Death Dis. 2023 Sep 8;14(9):600. 3. Madai S, et al. Activation of the hypoxia-inducible factor pathway protects against acute ischemic stroke by reprogramming central carbon metabolism. Theranostics. 2024 Apr 29;14(7):2856-2880. |
| 保存条件: |
-80°C 6个月;-20°C 1个月 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.195 ml |
10.977 ml |
21.953 ml |
| 5 mM |
0.439 ml |
2.195 ml |
4.391 ml |
| 10 mM |
0.22 ml |
1.098 ml |
2.195 ml |
| 50 mM |
0.044 ml |
0.22 ml |
0.439 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。 |