cIAP1 Ligand-Linker Conjugates 8 comprises an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound is specifically utilized for the purpose of SNIPER design[1].
GS-462808 is a late sodium current inhibitor of the cardiac Nav1.5 channel. GS-462808 had lower brain penetration and serendipitously lower activity at the brain isoforms.
PXS-4681A is a powerful, specific, and irreversible inhibitor of semicarbazide-sensitive amine oxidase (SSAO; VAP-1), with an oral activity and a Ki value of 37 nM. It exhibits exceptional selectivity towards related amine oxidases, ion channels, and seven-transmembrane domain receptors. Additionally, PXS-4681A demonstrates potent anti-inflammatory properties.
Chaetomellic acid A is a potent inhibitor of farnesyltransferase in isolated enzyme assays (IC50=55nM) but is inactive in whole cells. Inhibition of farnesyltransferase is selective over geranylgeranyltransferase I and II (IC50=92µM and 34µM respectively).
Doripenem is a broad-spectrum carbapenem antibiotic effective against both Gram-negative and Gram-positive bacteria, such as S. aureus, S. pneumoniae, E. coli, and K. pneumoniae, with minimum inhibitory concentrations (MICs) ranging from less than 0.015 to 0.3 µg/ml. It has been proven to reduce the viable bacteria count in mouse lung models of chronic P. aeruginosa respiratory tract infection at a dosage of 100 mg/kg per day. Doripenem operates by inhibiting bacterial cell wall synthesis through the formation of stable acyl-enzyme complexes with penicillin-binding proteins, leading to their inactivation. This compound has been utilized in various formulations for the treatment of bacterial infections.