DNAligase-IN-2 (compound 2) 是 LigA 的高效抑制剂,能够抑制全长 LigA 及截短酶 LigA:AD 的 DNA 非依赖性自发腺苷酸化活性,其 IC50 为 29 nM。此化合物显著抑制金黄色葡萄球菌的体外生长,对于金黄色葡萄球菌 (S. aureus) ATCC 29213、金黄色葡萄球菌 (S. aureus) ATCC 700699 的 MIC 值为 1 μg mL,而对大肠杆菌 (E. coli) ATCC 25922 的 MIC 值大于 64 μg mL。
HLI373 dihydrochloride is a potent Hdm2 inhibitor, efficiently restraining the ubiquitin ligase activity of Hdm2 and effectively prompting apoptosis in DNA-damaging agent-sensitive tumor cells[1]. Additionally, HLI373 dihydrochloride exhibits antimalarial activity[2].
Pinafide is a rodenticide and anti-protozoal agent. Pinafide shows strong cytostatic activity against both HeLa and KB cells and is moderately toxic to both mice and rats. It has been proved active against experimental tumors and shown to be inhibitor of two DNA viruses. Pinafide blocks cell growth by inhibiting DNA and RNA synthesis. It has been shown to bind to double-helical DNA by intercalation. Pinafide inhibited the activity of M. tuberculosis NAD⁺-dependent DNAligase A at concentrations of 50 uM. At the chemical screening was found that pinafide inhibited B-Myb transcriptional activity in luciferase assays. The cross placental-barrier studies showed that 3H-pinafide was present in the 14-day fetuses.