179461-52-0

PD 151746 acts as a cell-permeable calpain inhibitor which induce pertussis toxin (PTx)-sensitive chemotaxis in neutrophils and human monocytes. This results in an inhibition of inflammation.

This cell-permeable thiol-reactive agent (FW = 237.25 g/mol; CAS 179461- 52-0), also named (Z) -3- (5-fluoroindol-3-yl) -2-mercapto-2-propenoate, inhibits μ-calpain (Ki = 0.21 μM) decreases oxLDL-induced cytotoxicity, whereas the general caspase inhibitor BAF (t-butoxycarbonyl-Asp- methoxyfluoromethylketone) is without effect. Note that the structurally related inhibitor (Z) -3- (4-iodophenyl) -2-mercapto-2-propenoate does not appear to react at the active site, instead targeting the calcium ion binding site. (See also (Z) -3- (4-Iodophenyl) -2-mercapto-2-propenoate)

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