2243453-32-7

PARP1/2/TNKS1/2-IN-1 (Compound I-9) is a dual PARP-1, PARP-2, TNKS1 and TNKS2 inhibitor with IC50 values of 0.25 nM, 1.2 nM, 13.5 nM and 4.15 nM against PARP-1, PARP-2, TNKS1 and TNKS2, respectively. PARP1/2/TNKS1/2-IN-1 exhibits favorable synergistic antitumor efficacy and induces apoptosis[1].

PARP-1: 0.25 nM (IC₅₀); PARP-2: 1.2 nM (IC₅₀); TNKS2: 4.15 nM (IC₅₀); TNKS1: 13.5 nM (IC₅₀)

[1] Xu Y, et al. Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy. Eur J Med Chem. 2022 Jul 5;237:114417. DOI:10.1016/j.ejmech.2022.114417