OUL245

Names

[ Name ]:
OUL245

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> PARP

Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

[Target]

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)

[In Vitro]

OUL245 (1 μM; 10-12 d) 与其他衍生物不同，它不能拯救过表达 PARP10 的细胞，使其免于 ADP 核糖化依赖的细胞死亡[1]。药代动力学分析[1] water solubility μg/mL GI Papp×10-6 cm/s (RM %) BBB Papp×10-6 cm/s (RM %) metabolic stablity % stab in human plasma stab. in MeOH stab in PBS pH 7.4 24.91 0.019 0.164 95.05 >24 >24 >24

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₈H₅N₃OS

[ Molecular Weight ]:
191.21

Related Compounds

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