DNA Ligase Inhibitor

L67 (DNA Ligase Inhibitor) is a competitive inhibitor of human DNA ligases I and III with an IC50 of 10 μM.

L82 is a DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM) that is selective and non-competitive.L82 expresses anti-proliferative activity against breast cancer cells.

β-Lapachone (ARQ-501) is a specific DNA topoisomerase I inhibitor, and no inhibitory activities against DNA topoisomerase II or ligase.

DNA ligase-IN-1 (Compound 1) is an inhibitor of the bacterial NAD+-dependent DNA ligase (LigA) and effectively suppresses the in vitro growth of Staphylococcus aureus.

DNA ligase-IN-2 (compound 2) acts as a potent LigA inhibitor, effectively hindering the DNA-independent spontaneous adenylation activity of full-length LigA and the truncated enzyme LigA:AD with an IC50 of 29 nM. It also significantly suppresses the in vitro growth of Staphylococcus aureus, showing MIC values of 1 μg mL for S. aureus ATCC 29213 and S. aureus ATCC 700699, while the MIC for Escherichia coli (E. coli) ATCC 25922 is >64 μg mL.

HLI373 is an efficacious Hdm2 inhibitor, an ubiquitin ligase (E3), effective in inducing apoptosis of several tumor cells sensitive to DNA-damaging agents [1], and also shows prominent antimalarial activity [2].

SCR7, a specific DNA Ligase IV inhibitor, blocks nonhomologous end-joining (NHEJ).

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].

L189 is a human DNA ligase inhibitor, inhibits hLigI III IV (IC50: 5 9 5 μM).

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 DNA ligase 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.

MEL24, an Mdm2 E3 ligase inhibitor, diminishes cell viability and enhances sensitivity to DNA-damaging agents in a p53-dependent manner, suggesting its potential for in vitro antitumor research [1].

SCR130 (1,7,9-Triazaspiro[4.5]dec-1-ene-6,10-dione, 2,4-bis(4-chlorophenyl)-8-thioxo-) is enzyme inhibition, antiproliferative effects and antifungal activity.