1023814-45-0

OUL245 is a 7-Hydroxy derivative, and a selectively PARP2 inhibitor (IC50=44 nM). OUL245 also inhibits other PARP and TNKS enzymes with IC50s of 2.9-8.8 μM[1].

PARP2: 44 nM (IC₅₀); PARP-1: 570 nM (IC₅₀); PARP3: 8.8 μM (IC₅₀); PARP4: 6.0 μM (IC₅₀); TNKS1: 1.6 μM (IC₅₀); TNKS2: 370 μM (IC₅₀); PARP10: 2.9 μM (IC₅₀); PARP14: 6.7 μM (IC₅₀); PARP15: 2.0 μM (IC₅₀)

[1] Murthy S, et al. [1,2,4]Triazolo[3,4-b]benzothiazole Scaffold as Versatile Nicotinamide Mimic Allowing Nanomolar Inhibition of Different PARP Enzymes. J Med Chem. 2023 Jan 4. DOI:10.1021/acs.jmedchem.2c01460