IWP L6 (IWPL6, IWP-L6, Porcn Inhibitor III)是高活性、强效的Porcupin (Porcn)抑制剂(EC50为0.5 nM),Porcupin是催化Wnt蛋白棕榈酰化的酶,IWP L6在高浓度下可以阻断Wnt信号的传导。IWP L6在人血浆中的稳定性高于大鼠小鼠。在HEK293细胞中,IWP-L6可显著抑制dishevelled 2 (Dvl2)的磷酸化。
参考文献
[1] Wang X, et al. The development of highly potent inhibitors for porcupine. J Med Chem. 2013 Mar 28;56(6):2700-4. doi: 10.1021/jm400159c. Epub 2013 Mar 19. PMID: 23477365; PMCID: PMC3631274.
[2] Volpini X, et al. Wnt Signaling Plays a Key Role in the Regulation of the Immune Response and Cardiac Damage during Trypanosoma cruzi Infection. ACS Infect Dis. 2021 Feb 11. doi: 10.1021/acsinfecdis.0c00590. Epub ahead of print. PMID: 33573383.
[3] Dodge ME, et al. Diverse chemical scaffolds support direct inhibition of the membrane-bound O-acyltransferase porcupine. J Biol Chem. 2012 Jun 29;287(27):23246-54. doi: 10.1074/jbc.M112.372029. Epub 2012 May 15. PMID: 22593577; PMCID: PMC3391103.
冰袋运输。粉末直接保存于-20℃,有效期2年。建议分装后-20℃干燥保存,避免反复冻融。