Glutaminyl cyclases-IN-1  (Synonyms: IsoQC-IN-1)

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].

IC₅₀: 12 nM (human QC), 73 nM (iso QC)^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

478.61

C₂₅H₃₀N₆O₂S

COC1=C(C=CC(CN2C=NC3=CC(C4=NN=C(S4)N)=CC=C32)=C1)OCCCN5CCCCC5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.