OUL232

Modify Date: 2024-04-09 17:35:39

OUL232 Structure
OUL232 structure
Common Name OUL232
CAS Number 943119-42-4 Molecular Weight 250.28
Density N/A Boiling Point N/A
Molecular Formula C10H10N4O2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of OUL232


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].

 Names

Name OUL232

 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
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