PD 151746 179461-52-0

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Molecular Weight:

237.25 PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain.






Biological Activity


In SY5Y cells, PD151746 effectively attenuates the SLLVY-AMC hydrolysis induced by maitotoxin. In HMEC-1 cells, PD 151746 decreases cytotoxicity induced by oxidized low-density lipoprotein (oxLDL).






Protease Assays


The calpain microplate assay is carried out as followed. Briefly, a
mixture containing 0.5 mg/ml casein, 20 mM DTT, 50 mM Tris-HCl (pH 7.4),
0.01 unit purified, μ-calpain (human erythrocytes) or m-calpain (rabbit
skeletal muscle) (about 0.08-0.12 ,ug) in the presence of various
concentrations of an inhibitor.


CaCl2 (4 mM) is added to a
microtiter plate (250 ,tl) and incubated for 60 min at 25. The samples
are then processed for colorimetric development and read on a Molecular
Devices Thermomax microplate reader at an absorbance of 595 nm. Apparent
Ki values are calculated.

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Product Categories : Proteases > Cysteine Protease Inhibitor