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商品描述
| Source | M.W. | 396.4 | CAS No. | 1243244-14-5 | |
|---|---|---|---|---|---|
| Structural Info | |||||
| Formulation | Powder | ||||
| Reconstitution | Before reconstitution, werecommend a brief spin to drive down any material dislodged from the bottom ofthe tube. The compound is soluble inDMSO. | ||||
| Stability | The powder is stable for atleast 2 year if stored at -20 °C. The dissolved compound is stable for at least 1 month at 4 °C, butshould 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 isa potent and specific inhibitor of O-acyltransferase Porcupine (Porcn)that acylates Wnt proteins required for their biological activities. The structure of LGK974 was recentlypublished (Ref. 1). Not only morepotent than the IWP1,2,3,4 Porcn inhibitors (Ref. 2), LGK974 is also suitablefor in vivo studies and is currentlyin the Phase I clinical trials to treat cancers.Ref 1. Discovery of LGK974: Aselective Porcupine inhibitor targeting Wnt signaling in cancer. Shifeng Pan(Novartis), 2013 AACR Annual Meeting.Ref2. Chen B., et al. Smallmolecule-mediated disruption of Wnt-dependent signaling in tissue regenerationand cancer. Nat Chem Biol. 2009;5(2):100-7.
