TST1N-224

Description

TST1N-224 is a potent response regulator VraRC inhibitor. TST1N-224 can disrupt VraRC-DNA complex formation IC50=60.2 ?M . TST1N-224 exhibits interference with VraRC binding to its cognate DNA through a fast-on-fast-off binding mechanism KD=23.4 ?M . TST1N-224 predominantly interacts with the ?9- and ?10-helixes of the DNA-binding domain of VraR. TST1N-224 inhibits the growths of S. aureus SA; MIC 126 ?M, Methicillin-resistant S. aureus MRSA; MIC 126 ?M, and Vancomycin-intermediate S. aureus VISA; MIC=63 ?M . TST1N-224, an antimicrobial agent, evidently enhances the susceptibility of VISA to both Vancomycin HY-B0671 and Methicillin HY-B0974 .