Notum-IN-2
Notum-IN-2 is a partially brain-penetrant Notum carboxyl-esterase inhibitor with an IC50 of 18 nM. Notum-IN-2 can be used as a chemical tool for exploring Wnt signalling in cells.
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- CAS. Nr.: 2411969-28-1
- Formel: C9H4ClF3N2O2
- Molecular Weight:264.59
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Notum-IN-2 (6ZVL) potently inhibits Notum carboxyl-esterase with an IC50 of 0.018 μM, achieving a 640-fold potency increase from its parent fragment hit[1].
Notum-IN-2 (0.3 nM- 10 μM) shows an activation of Wnt signaling (EC50 = 3500 nM) in a cell-based TCF/LEF reporter gene (Luciferase) assay through the inhibition of Notum in a concentration-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL6 mice (male)[2]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Had a rapid absorption and modest BBB penetration.
Chemical Information
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CAS. Nr. 2411969-28-1
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Molecular Weight 264.59
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Formel C9H4ClF3N2O2
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SMILES
O=C1OC(C2=CC(C(F)(F)F)=C(Cl)C=C2)=NN1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Li ASM, et al. Discovery of Nanomolar DCAF1 Small Molecule Ligands. J Med Chem. 2023;66(7):5041-5060. [Content Brief]
[2]. Mahy W, et al. 5-Phenyl-1,3,4-oxadiazol-2(3H)-ones Are Potent Inhibitors of Notum Carboxylesterase Activity Identified by the Optimization of a Crystallographic Fragment Screening Hit. J Med Chem. 2020 Nov 12;63(21):12942-12956. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Notum-IN-2 Related Classifications
HY-182402 Related Classifications
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