Description
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.
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
Additional Information
Storage Condition: |
-20°C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
48 months |