| Bioactivity | 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[1]. |
| Target | IC50: 12 nM (human QC), 73 nM (iso QC) |
| Invitro | 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[1]. |
| Name | Glutaminyl cyclases-IN-1 |
| Formula | C25H30N6O2S |
| Molar Mass | 478.61 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |