DNA Ligase Inhibitor

SCR7 pyrazine is a DNA ligase IV inhibitor that blocks nonhomologous end-joining (NHEJ) in a ligase IV-dependent manner. SCR7 pyrazine increases the efficiency of Cas9-mediated homology-directed repair (HDR). SCR7 pyrazine induces cell apoptosis and has anticancer activity.

L67 (DNA Ligase Inhibitor) is a competitive DNA ligase inhibitor that effectively inhibits DNA ligases I/III (both IC₅₀ are 10 μM). L67 can cause nuclear DNA damage by reducing levels of mitochondrial DNA and increasing levels of mitochondrially-generated ROS. L67 also activates the Caspase 1-dependent apoptosis pathway in cancer cells, can be used in cancer research.

L82 is a selective and uncompetitive DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC₅₀=12 μM). L82 shows anti-proliferative activity to breast cancer cells.

L82-G17 is an uncompetitive DNA ligase I (Lig I)-selective inhibitor. L82-G17 inhibits the third step of the ligation reaction, phosphodiester bond formation. L82-G17can be used as a probe of the catalytic activity.

L189 is a DNA ligase inhibitor. L189 has inhibition effect for DNA Ligase I, III and IV with IC₅₀ values of 5 μM, 9 μM and 5 μM, respectively. L189 has no cytotoxicity and individually increase cell death. L189 can be used for the research of cancer.

Bleomycin B2 (Phleomycin D2) sulfate is a selective antitumor and antibacterial agent that induces DNA strand breaks and inhibits DNA ligase activity. The optimal pH for the activity of Bleomycin B2 sulfate is 9.1, and its efficacy is enhanced by thiol compounds or hydrogen peroxide. Bleomycin B2 sulfate undergoes enzymatic inactivation via bleomycin-inactivating enzymes, exhibits selective retention in squamous cell carcinoma, and is inactivated most rapidly in liver and kidney homogenates. Bleomycin B2 sulfate can be applied in research related to squamous cell carcinoma and other relevant studies.

DNA relaxation-IN-1 (Compound 27) is a DNA ligase 1 DNA Lig1) inhibitor. DNA relaxation-IN-1 inhibits DNA ligation and disrupts the DNA relaxing activity of DNA Lig1. DNA relaxation-IN-1 induces Apoptosis. DNA relaxation-IN-1, in combination with Topotecan (HY-13768), exhibits synergistic antiproliferative effects against colorectal cancer.

DNA ligase-IN-2 (compound 2) is a potent LigA inhibitor and inhibits the DNA-independent autoadenylation activity of both full-length LigA and a truncated enzyme, LigA:AD (IC₅₀=29 nM). DNA ligase-IN-2 effectively inhibits the growth of Staphylococcus aureus in vitro, with MIC valuse of 1, 1, and >64 μg/mL for S. aureus ATCC 29213, S. aureus ATCC 700699 and E. coli ATCC 25922, respectively.

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