LGK974 | 2645

LGK-974 is a potent and specific inhibitor of Porcupine (porcn), a Wnt-specific acyltransferase (IC₅₀ = ~0.4 nM). GK974 potently inhibits Wnt signaling, has strong efficacy in rodent tumor models, and is well-tolerated. In addition, head and neck cancer cell lines with loss-of-function mutations in the Notch signaling pathway have a high response rate to LGK974.

LGK-974 is a potent and specific inhibitor of Porcupine (porcn), a Wnt-specific acyltransferase (IC₅₀ = ~0.4 nM). GK974 potently inhibits Wnt signaling, has strong efficacy in rodent tumor models, and is well-tolerated. In addition, head and neck cancer cell lines with loss-of-function mutations in the Notch signaling pathway have a high response rate to LGK974.

2645 | LGK974 DataSheet

Alternate Name/Synonyms: 2-(2',3-dimethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide

Appearance: Crystalline solid

Formulation: N/A

CAS Number: 1243244-14-5

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₃H₂₀N₆O

Molecular Weight: 396.44

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO (~ 35 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent Porcupine (porcin) inhibitor

MDL Number: N/A

PubChem CID: 46926973

SMILES: CC1=C(N=CC(=C1)CC(=O)NC2=NC=C(C=C2)C3=NC=CN=C3)C4=CC(=NC=C4)C

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)

InChi Key: XXYGTCZJJLTAGH-UHFFFAOYSA-N