| 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.
StemRD 是美国一家聚焦于尖端干细胞研究的公司，拥有蛋白表达和纯化方面的专利技术，使StemRD能够保证高效的生产那些用传统方法很难得到的重要干细胞因子。StemRD 拥有被美国FDA认证的可用于GMP生产治疗型多肽的设施。StemRD的实验室也拥有包括组织培养、细胞处理、超离心、超过滤、FPLC、HPLC和LC/MS等一系列先进设备。
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