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[1].
L82-G17 (200 μM, 30 min) has selective uncompetitive inhibitory effect for LigI[1].
L82-G17 (0-100 μM) increases LigI binding to non-ligatable nicked DNA binding[1].
L82-G17 inhibits step 3 of the ligation reaction, phosphodiester bond formation[1].
L82-G17 (0-100 μM) inhibits DNA synthesis, cell viability and s induces DNA damage[1].
Cell Viability Assay[1]
| Cell Line: | HeLa cells |
| Concentration: | 0-30 μM |
| Incubation Time: | 5 days |
| Result: | Reduced cell number by about 70% at 20 μM. |
Cell Proliferation Assay[1]
| Cell Line: | CH12F3 WT and CH12F3δ/δ cells |
| Concentration: | 0-100 μM |
| Incubation Time: | 72 h |
| Result: | Had great effect on the proliferation and survival of the parental CH12F3 cells. |
[1]. Timothy R L Howes, et al. Structure-activity relationships among DNA ligase inhibitors: Characterization of a selective uncompetitive DNA ligase I inhibitor. DNA Repair (Amst). 2017 Dec;60:29-39.