TST1N-224

TST1N-224 is a potent response regulator VraRC inhibitor. TST1N-224 can disrupt VraRC-DNA complex formation (IC50=60.2 μM) . TST1N-224 exhibits interference with VraRC binding to its cognate DNA through a fast-on-fast-off binding mechanism (KD=23.4 μM) . TST1N-224 predominantly interacts with the α9- and α10-helixes of the DNA-binding domain of VraR. TST1N-224 inhibits the growths of S. aureus (SA; MIC>126 μM), Methicillin-resistant S. aureus (MRSA; MIC>126 μM), and Vancomycin-intermediate S. aureus (VISA; MIC=63 μM) . TST1N-224, an antimicrobial agent, evidently enhances the susceptibility of VISA to both Vancomycin (HY-B0671) and Methicillin (HY-B0974) [1].

Product Specifications

CAS Number

[50566-97-7]

UNSPSC

12352211

Target

Antibiotic; Bacterial

Type

Reference compound

Related Pathways

Anti-infection

Field of Research

Infection

Assay Protocol

https://www.medchemexpress.com/tst1n-224.html

Smiles

O=S(CCOCC1SSC(COCCS(=O)(O)=O)CSSC1)(O)=O

Molecular Formula

C10H20O8S6

Molecular Weight

460.65

References & Citations

[1]Ying-Chu Hsu, et al. Combatting Antibiotic-Resistant Staphylococcus aureus: Discovery of TST1N-224, a Potent Inhibitor Targeting Response Regulator VraRC, through Pharmacophore-Based Screening and Molecular Characterizations. J Chem Inf Model. 2024 Aug 12;64 (15) :6132-6146.