| 产品描述: | AX20017 is a small-molecule protein kinase G (PknG) inhibitor with an IC50 of 0.39 μM. |
| 靶点: |
IC50: 0.39 μM (PknG) |
| 体外研究: |
The compound AX20017 inhibitor is bound deep within a narrow pocket formed by the inter lobe cleft of the PknG domain. The main chain Glu233:O and Val235:NH of PknG form hydrogen bonds with AX20017.AX20017 results in mycobacterial transfer to lysosomes and killing of the mycobacteria. AX20017 does not affect the human kinases, whereas the activity of PknG is effectively inhibited. AX20017 does not affect cellular morphology, membrane ruffling, or macropinocytosis |
| 参考文献: |
1. Walburger A, et al. Protein kinase G from pathogenic mycobacteria promotes survival within macrophages. Science. 2004 Jun 18;304(5678):1800-4. 2. Santhi N, et al. Insights from the molecular docking of withanolide derivatives to the target protein PknG from Mycobacterium tuberculosis. Bioinformation. 2011;7(1):1-4. 3. Scherr N, et al. Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis. Proc Natl Acad Sci U S A. 2007 Jul 17;104(29):12151-6. |
| 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 |
3.783 ml |
18.915 ml |
37.83 ml |
| 5 mM |
0.757 ml |
3.783 ml |
7.566 ml |
| 10 mM |
0.378 ml |
1.891 ml |
3.783 ml |
| 50 mM |
0.076 ml |
0.378 ml |
0.757 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。 |