α-chymase

Chymase-IN-1 is a selective, orally active inhibitor of human mast cell chymase (IC50: 29 nM).

Chymase-IN-2 is a modulator of chymase.

CH 5450 (Z-Ile-Glu-Pro-Phe-Ome) is a short peptide inhibitor of chymase in the human heart.

Fulacimstat (BAY1142524) (BAY1142524) is a chymase inhibitor, with IC50s of 3, 4 nM for hamster and human chymase enzyme, respectively.

Chymase is a proteolytic enzyme predominantly found in mast cells (MC), fibroblasts, and vascular endothelial cells. It is released into the extracellular matrix in response to inflammatory signals, tissue damage, and cellular stress. Chymase also plays a role in the generation of angiotensin II (Ang II), making it significant for cardiovascular disease research.

Chlorobenzothiazolinone inhibits recombinant human chymase using bis(succinoyl-L-alanyl-L-prolyl-L-phenylalanylamide) as substrate after 1 hr by fluorescence assay with activity value of 90 μM.

TY-51469 is an inhibitor of chymase (IC50s for simian and human chymases: 0.4 and 7.0 nM, respectively).

Iptacopan (LNP023) is an inhibitor with high affinity to factor B, with a KD value of 7.9 nM and an IC50 value of 10 nM.