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^[1][2].

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.

Notum-IN-2 (6ZVL) (10 mg/kg; p.o.; single dose) has a rapid absorption and modest BBB penetration in male C57BL6 mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

264.59

C₉H₄ClF₃N₂O₂

2411969-28-1

O=C1OC(C2=CC(C(F)(F)F)=C(Cl)C=C2)=NN1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.