OUL245
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.
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- CAS No.: 1023814-45-0
- Formule: C8H5N3OS
- Masse moléculaire:191.21
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[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) |
In Vitro
OUL245 (1 μM; 10-12 d) unlike other derivatives, does not save cells overexpressing PARP10 from ADP ribosylation-dependent cell death[1].
Pharmacokinetic Analysis[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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1023814-45-0
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Masse moléculaire 191.21
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Formule C8H5N3OS
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SMILES
C1=CC2=C(C=C1O)SC3=NN=CN23
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)