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ARUK3001185

Chemical Structure : ARUK3001185

CAS No.: 2411969-39-4

ARUK3001185 (ARUK 3001185)

Catalog No.: PC-72827Not For Human Use, Lab Use Only.

ARUK3001185 is a potent, selective, brain-penetrant inhibitor of Wnt-deactivating enzyme Notum carboxylesterase activity with IC50 of 6.7 nM in OPTS biochemical assay.

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Biological Activity

ARUK3001185 is a potent, selective, brain-penetrant inhibitor of Wnt-deactivating enzyme Notum carboxylesterase activity with IC50 of 6.7 nM in OPTS biochemical assay.
ARUK3001185 restored Wnt signaling in the presence of Notum (EC50 110 nM) in a in a cell-based TCF/LEF (Luciferase) reporter assay.
ARUK3001185 demonstrated high selectivity against a panel of serine hydrolases, kinases, and representative drug targets.
ARUK3001185 displayed good brain penetration suitable for oral dosing in rodent models of disease.

Physicochemical Properties

M.Wt 282.047
Formula C9H4Cl2F3N3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(2,4-dichloro-3-(trifluoromethyl)phenyl)-1H-1,2,3-triazole

References

1. William Mahy, et al. J Med Chem. 2020 Nov 12;63(21):12942-12956.

2. Elliott D Bayle, et al. J Med Chem. 2021 Apr 22;64(8):4289-4311.

3. Zhao Y, et al. Future Med Chem. 2021 Jun;13(11):1001-1015.

4. University of Oxford: WO2020043866 (2020).

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