PD 150,606

Uses

A cell-permeable, non-competitive, selective non-peptide calpain inhibitor [K_i = 210 nM for calpain-1 and 370 nM for calpain-2] directed towards the calcium binding sites of calpain. Exhibits high specificity for calpains relative to other proteases, such as cathepsin B and cathepsin L. Does not shield calpain against inactivation by the active-site inhibitor trans-(epoxysuccinyl)-L-leucyl-amido-3-methylbutane. Reportedly prevents dexamethasone-induced apoptosis in thymocytes.
A cell-permeable, selective non-peptide calpain inhibitor (K_i = 210 nM for calpain I and 370 nM for calpain II) directed towards the calcium- binding sites of calpain. Exhibits high specificity for calpains relative to other proteases, such as cathepsin B and L. PD 150606 is a non-competitive inhibitor with respect to the substrate and does not shield calpain against inactivation by the active-site inhibitor trans-(epoxysuccinyl)-L-leucyl-amido-3-methylbutane. Reportedly prevents dexamethasone-induced apoptosis of thymocytes.

Definition

ChEBI: (Z)-3-(4-iodophenyl)-2-mercaptoacrylic acid is 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). It has a role as a calpain inhibitor and an apoptosis inhibitor. It is an organoiodine compound, a member of cinnamic acids and a thioenol. It is functionally related to a trans-cinnamic acid.

Biological Activity

Cell permeable: yes', 'Primary Target
Calpain-1', 'Product does not compete with ATP.', 'Reversible: no', 'Target Ki: 210 nM for calpain-1 and 370 nM for calpain-2

storage

+4°C

Raw materials

Preparation Products