MP-1 is a covalent inhibitor of fumarate hydratase (FH) that exhibits cytotoxicity dependent on FH. MP-1 engages a functional cysteine in the Zn-finger domain of the tRNA methyltransferase enzyme TRMT1.
IMP-1700 is an inhibitor of bacterial DNA repair.1It potentiates the activity of the quinolone antibiotic ciprofloxacin against methicillin-resistantS. aureus(MRSA) with a combination index value of 0.7. IMP-1700 inhibits the ciprofloxacin-induced bacterial SOS response, a process that repairs DNA damage, in a reporter assay in a concentration-dependent manner. It is also active againstE. coli, as well as methicillin-resistant and -sensitive S. aureus, when used alone (EC50s = 0.5, 0.21, and 3.8 μM, respectively). 1.Lim, C.S.Q., Ha, K.P., Clarke, R.S., et al.Identification of a potent small-molecule inhibitor of bacterial DNA repair that potentiates quinolone antibiotic activity in methicillin-resistant Staphylococcus aureusBioorg. Med. Chem.27(20)114962(2019)
MP135 is a Novel μ−δ Opioid Receptor Heteromer-Selective Agonist. MP135 maintains untoward side effects such as respiratory depression and reward behavior; together, these results suggest that optimization of MP135 is necessary for the development of therapeutics that suppress the classical side effects associated with conventional clinical opioids.