Small-molecule inhibitor: PD151746
Name
- Common name
- PD151746
Inhibition
- Peptidases inhibited
- Inhibits calpain-1. There is 20-fold selectivity for calpain-1 (Ki 0.26 uM) over calpain-2: Ki 5.33 uM) (Wang et al., 1996). Inhibition of other cysteine peptidase (e.g. papain, and cathepsin B) and non-cysteine peptidases tested was insignificant.
- Mechanism
- Inhibition is reversible, presumably mechanistically similar to that of PD150606. It is likely that binding of the inhibitor to the calcium-binding sites disrupts the conformational changes that are necessary to activate the catalytic domain (Wang et al., 1996).
Chemistry
- CID at PubChem
- 5353866
- Structure
![[PD151746 (C02.001 inhibitor) structure ]](/merops/smi/structures/pd151746.gif)
- Chemical/biochemical name
- (E)-3-(5-fluoro-1H-indol-3-yl)-2-sulfanyl-prop-2-enoic acid; 3-(5-fluoro-3-indolyl)-2-mercapto-(Z)-2-propenoic acid
- Formula weight
- 237
- Related inhibitors
- PD150606 is another 2-mercapto-propenoic acid inhibitor of calpains.
