| 产品描述: | Glutaminyl cyclases-IN-1 (IsoQC-IN-1) is a potent glutaminyl cyclases (QC) inhibitor with IC50 values of 12 nM and 73 nM for human QC and isoQC, respectively. Glutaminyl cyclases-IN-1 can selectively interfere with the interaction of CD47/SIRPα through isoQC inhibition, and enhances the increased phagocytic activity of both THP-1 and U937 macrophages. |
| 靶点: |
IC50: 12 nM (human QC), 73 nM (iso QC) |
| 体外研究: |
Glutaminyl cyclases-IN-1 (compound 22b) (0-20 μM; 24 or 48 h; A549 and H1975) increases the phagocytic activity of both THP-1 and U937 macrophages in a dose-dependent manner in A549 and H1975 cells; decreases the surface expression level of αhCD47-CC2C6 without interfering in αhCD47-B6H12 binding with CD47. |
| 参考文献: |
1. Eunsun Park, et al. 2-Amino-1,3,4-thiadiazoles as Glutaminyl Cyclases Inhibitors Increase Phagocytosis through Modification of CD47-SIRPα Checkpoint. ACS Med. Chem. Lett. 2022. |
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.089 ml |
10.447 ml |
20.894 ml |
| 5 mM |
0.418 ml |
2.089 ml |
4.179 ml |
| 10 mM |
0.209 ml |
1.045 ml |
2.089 ml |
| 50 mM |
0.042 ml |
0.209 ml |
0.418 ml |
|
| 注意: |
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