JCP174

JCP174 is an inhibitor of palmitoyl protein thioesterase-1 (TgPPT1), a depalmitoylase in the parasite T. gondii.¹ JCP174 enhances invasion of Toxoplasma tachyzoites into BSC-1 host cells, increasing the number of attached and invaded parasites when used at a concentration of 50 µM, enhancing plaque formation at concentrations of 0.5 and 50 µM, and increasing gliding motility. JCP174 is also an inhibitor of porcine pancreatic elastase and human leukocyte elastase.^2,3

WARNING This product is not for human or veterinary use.

1. Child, M.A., Hall, C.I., Beck, J.R., et al. Small-molecule inhibition of a depalmitoylase enhances Toxoplasma host-cell invasion. Nat. Chem. Biol. 9(10), 651-656 (2013).

2. Powers, J.C., Oleksyszyn, J., Narasimhan, S.L., et al. Reaction of porcine pancreatic elastase with 7-substituted 3-alkoxy-4-chloroisocoumarins: Design of potent inhibitors using the crystal structure of the complex formed with 4-chloro-3-ethoxy-7-guanidinoisocoumarin. Biochemistry 29(12), 3108-3118 (1990).

3. Kerrigan, J.E., Oleksyszyn, J., Kam, C.-M., et al. Mechanism-based isocoumarin inhibitors for human leukocyte elastase. Effect of the 7-amino substituent and 3-alkoxy group in 3-alkoxy-7-amino-4-chloroisocoumarins on inhibitory potency. J. Med. Chem. 38(3), 544-552 (1995).