1023814-45-0

1023814-45-0 structure

1023814-45-0 structure

Name: OUL245
Chemical Name: OUL245
CAS Number: 1023814-45-0
Molecular Formula: C₈H₅N₃OS
Molecular Weight: 191.21
Catalog: Signaling Pathways Cell Cycle/DNA Damage PARP
Create Date: 2023-04-03 17:12:17
Modify Date: 2024-04-03 16:34:31
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].

Name	OUL245

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.

Molecular Formula	C₈H₅N₃OS
Molecular Weight	191.21