|Reconstitution||Before reconstitution, we recommend a brief spin to drive down any material dislodged from the bottom of the tube. The compound is soluble in DMSO.|
|Stability||The powder is stable for at least 2 year if stored at -20 °C. The dissolved compound is stable for at least 1 month at 4 °C, but should be stored in aliquots at -20 °C for longer term. Protect from light.|
|Purity||Greater than 99% as determined by LC/MS analysis.|
|Biological Activity||In a co-culture assay measuring the activation of the TCF reporter gene by Wnt3a-secreting cells, this compound gives IC50 of 0.2 to 0.6 nM.|
|Country of Origin||USA|
LGK974 is a potent and specific inhibitor of O-acyltransferase Porcupine (Porcn) that acylates Wnt proteins required for their biological activities. The structure of LGK974 was recently published (Ref. 1). Not only more potent than the IWP1,2,3,4 Porcn inhibitors (Ref. 2), LGK974 is also suitable for in vivo studies and is currently in the Phase I clinical trials to treat cancers.
Ref 1. Discovery of LGK974: A selective Porcupine inhibitor targeting Wnt signaling in cancer. Shifeng Pan (Novartis), 2013 AACR Annual Meeting.
Ref 2. Chen B., et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009;5(2):100-7.