OUL232

Names

[ Name ]:
OUL232

Biological Activity

[Description]:

OUL232 is a potent inhibitor of mono-ARTs PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15. OUL232 is the most potent PARP10 inhibitor described to date (IC50=7.8 nM), as well as the first PARP12 inhibitor ever reported[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> PARP

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

[Target]

PARP7:83 nM (IC50)

PARP10:7.8 nM (IC50)

PARP14:300 nM (IC50)

PARP15:56 nM (IC50)

PARP1:15 μM (IC50)

PARP2:10 μM (IC50)

PARP3:50 μM (IC50)

PARP4:11 μM (IC50)

TNKS1:5.4 μM (IC50)

TNKS2:10 μM (IC50)

PARP11:240 nM (IC50)

PARP12:160 nM (IC50)

PARP16:3.4 μM (IC50)

[In Vitro]

OUL232 (化合物 27) (1 μM; 10-12 d) 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 12.60 0.144 0.143 99.11 >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 ]:
C₁₀H₁₀N₄O₂S

[ Molecular Weight ]:
250.28