3-(4-Iodophenyl)-2-mercapto-(Z)-2-propenoic acid

PD-150606 (179528-45-1) is a selective, cell-permeable non-peptide calpain inhibitor (Ki for μ- and m-calpains = 0.21 and 0.37 μM respectively). Acts at the calcium binding site of calpain rather than the substrate-binding site. Inhibits calpain activity in two intact cell systems. Attenuates hypoxic/hypoglycemic injury to cerebrocortical neurons in culture and excitotoxic injury to Purkinje cells in cerebellar slices.1 PD-150606 displays cytoprotective effects in oxidant- and calcium ionophore-induced cell death.2 Some protective effects may be due to inhibition of MMP activity.3

PD 150606 is a novel mercaptoacrylate based compound and a potent inhibitor of Ca2+-dependent activation of calpain-1, a Ca2+-activated cytosolic cysteine protease. PD 150606 may potentially be developed as an anti-inflammatory agent. Neuroprotective product.

ChEBI: An organoiodine compound that is acrylic acid in which the vinylic hydrogens at positions 2 and 3 are replaced by mercapto and 4-iodophenyl groups respectively (the Z geoisomer).

PD 150606 is a selective; cell-permeable; non-peptide; uncompetitive calpain inhibitor.

Store at -20°C

[1] K K WANG. An alpha-mercaptoacrylic acid derivative is a selective nonpeptide cell-permeable calpain inhibitor and is neuroprotective.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1996, 93 13: 6687-6692. DOI:10.1073/pnas.93.13.6687
[2] S L WATERS. Calpains mediate calcium and chloride influx during the late phase of cell injury.[J]. Journal of Pharmacology and Experimental Therapeutics, 1997, 283 3: 1177-1184.
[3] MOHAMMAD A.M. ALI . Calpain inhibitors exhibit matrix metalloproteinase-2 inhibitory activity[J]. Biochemical and biophysical research communications, 2012, 423 1: Pages 1-5. DOI:10.1016/j.bbrc.2012.05.005