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.
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].
References:
[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.