TDP1 Inhibitor-2 (compound 5) is a potent inhibitor for TDP1 (tyrosyl-DNA phosphodiesterase 1), with an IC50 of 99 nM. TDP1 Inhibitor-2 also can inhibit SCAN1 (spinocerebellar ataxia syndrome with axonal neuropat), with an IC50 of 3.5 μM[1].
TDP1 Inhibitor-2 (compound 5) shows potent anti-TDP1 activity, low cytotoxicity and synergism with topotecan, an established Top1 anticancer agent[1].
[1]. Mamontova EM, et al. Identification of novel inhibitors for the tyrosyl-DNA-phosphodiesterase 1 (Tdp1) mutant SCAN1 using virtual screening. Bioorg Med Chem. 2020 Jan 1;28(1):115234.
















