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LGK974
- WNT974
Axon 4390
CAS:
1243244-14-5
Purity:
99%
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C23H20N6O
- MW: 396.45
Description
LGK974 is a potent and highly specific PORCN inhibitor with IC50 values of 1 nM (PORCN radioligand binding assay) and 0.4 nM (Wnt coculture assay). LGK974 potently inhibits Wnt signaling in vitro and in vivo, including reduction of the Wnt-dependent LRP6 phosphorylation and the expression of Wnt target genes, such as AXIN2.
More Information
| Parent CAS No. | 1243244-14-5 |
|---|---|
| Chemical Name | N-(5-(2-Pyrazinyl)-2-pyridyl)(2',3-dimethyl-2,4'-bipyridyl-5-yl)acetamide |
| SMILES | N1C=C(CC(NC2N=CC(C3N=CC=NC=3)=CC=2)=O)C=C(C)C=1C1C=CN=C(C)C=1 |
| MFCD | MFCD27501026 |
| InChi | InChI=1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30) |
| InChiKey | XXYGTCZJJLTAGH-UHFFFAOYSA-N |
| CID | 46926973 |
| Short Description | PORCN inhibitor |
References
- J Liu et al. Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974. Proc Natl Acad Sci U S A. 2013 Dec 10;110(50):20224-9.
- A Kalantary-Charvadeh et al. The porcupine inhibitor WNT974 provokes ectodermal lineage differentiation of human embryonic stem cells. Cell Biochem Funct. 2022 Jun;40(4):359-368.
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