PK150 (Sorafenib Analog)

Analog of the anticancer drug sorafenib. PK150 is a potent antibiotic. It shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus (MRSA), Vancomycin intermediate S. aureus (VISA) with MICs of 0.3, 0.3-1, 0.3 µM, respectively. PK150 did not induce in vitro resistance and shows oral bioavailability and in vivo efficacy. The mode of action includes the interference with menaquinone biosynthesis by inhibiting demethylmenaquinone methyltransferase and the stimulation of protein secretion by altering the activity of signal peptidase IB.