LGK-974

Catalog No. A12816

LGK974 is a highly potent, selective and orally bioavailable Porcupine inhibitor (Wnt signaling antagonist) with an IC50 <1 nM in the Wnt signaling reporter assay and Porcupine binding assay.
  • Yang JM, .et al. LGK974, a PORCUPINE inhibitor, mitigates cytotoxicity in an in vitro model of Parkinson's disease by interfering with the WNT/β-CATENIN pathway, Toxicology, 2018, Dec 1;410:65-72 PMID: 30205152
  • E Lemieux, .et al. Oncogenic KRAS signalling promotes the Wnt/β-catenin pathway through LRP6 in colorectal cancer, Oncogene, 2015, Sep 17; 34(38): 4914-4927 PMID: 25500543
Catalog Num A12816
M. Wt 396.44
Formula C23H20N6O
Purity >98%
Storage at -20°C 3 years Powder
CAS No. 1243244-14-5
Synonyms LGK974, LGK 974
SMILES CC1=C(N=CC(=C1)CC(=O)NC2=NC=C(C=C2)C3=NC=CN=C3)C4=CC(=NC=C4)C
LGK974 is a highly potent, selective and orally bioavailable Porcupine inhibitor (Wnt signaling antagonist) with an IC50 <1 nM in the Wnt signaling reporter assay and Porcupine binding assay.
Targets
Porcn (TM3 cells)
In vitro DMSO 79 mg/mL heating (199.27 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 25.22 mL 126.12 mL 252.24 mL
0.5 mM 5.04 mL 25.22 mL 50.45 mL
1 mM 2.52 mL 12.61 mL 25.22 mL
5 mM 0.5 mL 2.52 mL 5.04 mL

*The above data is based on the productmolecular weight 396.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.