LGK974

LGK974 (WNT974) is an experimental drug which acts as an inhibitor of the porcupine O-acyltransferase enzyme, which plays an important part in the growth of certain types of cancer, especially colorectal cancer, pancreatic cancer, hepatocellular carcinoma and head and neck cancers. It is in early stage clinical trials for a number of cancer types.^[1][2][3]

LGK974

Identifiers
IUPAC name 2-[5-methyl-6-(2-methylpyridin-4-yl)pyridin-3-yl]-N-(5-pyrazin-2-ylpyridin-2-yl)acetamide
CAS Number	210826-47-4
PubChem CID	46926973
IUPHAR/BPS	11167
DrugBank	DB12561
ChemSpider	30507712
UNII	U27F40013Q
ChEBI	CHEBI:78030
ChEMBL	ChEMBL3188386
PDB ligand	O50 (PDBe, RCSB PDB)
Chemical and physical data
Formula	C23H20N6O
Molar mass	396.454 g·mol−1
3D model (JSmol)	Interactive image
SMILES CC1=CC(=CN=C1C2=CC(=NC=C2)C)CC(=O)NC3=NC=C(C=C3)C4=NC=CN=C4
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) Key:XXYGTCZJJLTAGH-UHFFFAOYSA-N

LGK974 has recently shown promise in preclinical models of the ultra-rare disease sclerosteosis, providing an alternative to invasive surgeries commonly required to the management of pathologies.^[4]