TST1N-224

TST1N-224 is an effective VraRC inhibitor that disrupts the formation of the VraRC-DNA complex (IC50=60.2 μM) . It interferes with the binding of VraRC to its homologous DNA through a rapid binding mechanism (KD=23.4 μM) and primarily interacts with the DNA binding domain helices α9 and α10 of VraR. TST1N-224 inhibits the growth of Staphylococcus aureus (SA; MIC>126 μM), methicillin-resistant Staphylococcus aureus (MRSA; MIC>126 μM), and vancomycin-intermediate Staphylococcus aureus (VISA; MIC=63 μM) . As an antimicrobial, TST1N-224 significantly enhances the sensitivity of VISA to vancomycin and methicillin.