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.

INVA8001 is a highly selective and orally active chymase inhibitor, with IC50 values of 0.02 μM for human chymase and 0.03 μM for mouse mast cell protease 4 (mMCP-4). It exhibits IC50 values of 3.4 μM for bovine α-chymotrypsin and 32.1 μM for human cathepsin G, demonstrating over 1000-fold selectivity against other related serine proteases. In a mouse model of primary sclerosing cholangitis (PSC), INVA8001 inhibits mast cell activity, improves biliary pathology, alleviates cholestasis, and displays anti-inflammatory and anti-fibrotic properties.