TDP1 Inhibitor-2

Names

[ Name ]:
TDP1 Inhibitor-2

Biological Activity

[Description]:

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 neuropathy), with an IC50 of 3.5 μM[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

Research Areas >> Neurological Disease

[Target]

IC50: 0.099 ± 0.044 μM (TDP1), 3.5 ± 2.3 μM (SCAN1)[1]

[In Vitro]

TDP1 Inhibitor-2 (compound 5) shows potent anti-TDP1 activity, low cytotoxicity and synergism with topotecan, an established Top1 anticancer agent[1].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₁₄Cl₂O₅

[ Molecular Weight ]:
465.28

Related Compounds

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