Calpain Inhibitor

PD 151746 is a selective calpain-1 inhibitor with an IC₅₀ of 260 nM. PD 151746 binds μ-calpain Ca²⁺-binding sites, and shows selectivity over cathepsin B, papain, trypsin, thermolysin, and basal calcineurin. PD 151746 reduces Oxidized low-density lipoprotein (oxLDL)-induced cytotoxicity, apoptotic DNA fragmentation, and blocks IL-1α maturation. PD 151746 can be used for the research of atherosclerosis and psoriasis.

Dazcapistat (BLD-2660) is an orally active small-molecule inhibitor of calpain 1, 2, and 9 (calpain 1, 2, 9). Dazcapistat reduces the expression/production level of IL-6 in injured lung tissue and alleviates fibrosis. Dazcapistat exerts anti-fibrotic effects in various animal models of fibrosis in the skin, liver and lung. Dazcapistat can be used in research related to coronavirus disease 2019 (COVID-19) and idiopathic pulmonary fibrosis.

CAST-calpain-2 stabilizer-1 is a blood-brain barrier permeable stabilizer of CAST-calpain-2 interaction. CAST-calpain-2 stabilizer-1 shows no activity against GSK3. CAST-calpain-2 stabilizer-1 can be used in the research of Huntington's disease and tauopathies.

SNJ-1945 is an orally active, blood-brain barrier-penetrant Calpain inhibitor. SNJ-1945 inhibits Cathepsin L, Cathepsin B, and Ca²⁺ -independent proteases. SNJ-1945 suppresses ROS production and downregulates Cyclooxygenase-2 and Caspase-1. SNJ-1945 alleviates left ventricular systolic dysfunction, reduces cerebral ischemia-induced injury, and decreases the score of experimental autoimmune encephalomyelitis in mouse models. SNJ-1945 can be used in research related to post-cardiac arrest reperfusion injury, Parkinson's disease, multiple sclerosis, and proliferative retinopathy.

N-Acetyl-L-leucyl-L-leucyl-L-methional is a Calpain II inhibitor with an IC₅₀ of 0.24 μM against porcine Calpain II. N-Acetyl-L-leucyl-L-leucyl-L-methional forms a stable tetrahedral adduct with the thiol group at the active site of Calpain II, thereby inhibiting proteolytic activity. N-Acetyl-L-leucyl-L-leucyl-L-methionally inhibits cathepsins in a non-selective manner. N-Acetyl-L-leucyl-L-leucyl-L-methional reduces SARS-CoV-2 infection levels in human coronary artery endothelial cells in vitro. N-Acetyl-L-leucyl-L-leucyl-L-methional can be used in research related to cataracts and coronavirus infections.