parylation

Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1 2 (Kis: 1.2 0.85 nM).

COH34 (1-[(E)-(4-methylphenyl)sulfanyliminomethyl]naphthalen-2-ol) is a selective inhibitor of PARG with an IC50 of 0.37 nM and a Kd of 0.547 μM. COH34 prolongs PARylation at DNA lesions and traps DNA repair factors.

(rac)-Talazoparib ((rac)-BMN-673) (Compound 47) is an orally active inhibitor of PARP1 2, with Ki values of 1.2 nM and 0.87 nM, respectively. It inhibits cellular PARylation at an EC50 of 2.51 nM. This compound leads to the accumulation of DNA damage and suppresses the proliferation of BRCA1 2-mutated MX-1 and Capan-1 cells, with IC50 values of 0.3 nM and 5 nM, respectively. Additionally, (rac)-Talazoparib exhibits antitumor activity in mouse models.

2-Azido-NAD, an analog of NAD+, is utilized for visualizing the intracellular poly (ADP-ribosyl)ation (PARylation) process.