Wortmannin是一种真菌代谢物,高效、选择性抑制PI3K,IC50为3 nM,可抑制自噬体的形成,其抑制能力高于另外一种常用的PI3K抑制剂LY294002。Wortmannin对PI3K家族的选择性很小,对PI3K家族成员I、II、III的作用差不多,并抑制MLCK。Wortmannin对DNA-PK、ATM抑制的IC50分别为16 nM、150 nM。通过抑制PI3K/Akt信号转导级联通路,Wortmannin增强了辐射或血清饥饿诱发的细胞凋亡以及阻断细胞因子介导的抗凋亡效应。大鼠脂肪细胞中,wortmannin能够阻断胰岛素受体激活的许多短期代谢活动,而且不会影响胰岛素受体酪氨酸激酶活性。
与LY188011 (Cat#51413)联合使用时,Wortmannin显著促进细胞凋亡,并抑制肿瘤生长。
参考文献
[1] Liu et al. Wortmannin, a widely used phosphoinositide 3-kinase inhibitor, also potently inhibits mammalian polo-like kinase. Chem.Biol. 12: 99-107(2005).
[2] Rozina Akter, et al. Wortmannin induces MCF-7 breast cancer cell death via the apoptotic pathway, involving chromatin condensation, generation of reactive oxygen species, and membrane blebbing. Breast Cancer (Dove Med Press) 4: 103–113 (2012).
[3] Ng SS, et al. Wortmannin inhibits pkb/akt phosphorylation and promotes gemcitabine antitumor activity in orthotopic human pancreatic cancer xenografts in immunodeficient mice. Clin Cancer Res, 7(10): 3269-3275 (2001).
客户使用本产品发表的科研文献(部分)
- Lin D L, Yao H Y, Jia L H, et al. Phospholipase D‐derived phosphatidic acid promotes root hair development under phosphorus deficiency by suppressing vacuolar degradation of PIN‐FORMED2. New Phytol. 2020 Apr;226(1):142-15. IF: 7.299
- Wu J, Ni Y, Yang Q, et al. Long-term arsenite exposure decreases autophagy by increased release of Nrf2 in transformed human keratinocytes. Sci Total Environ. 2020 Sep 10;734:139425. IF: 6.551
冰袋运输。粉末直接保存于-25~-15℃,溶于溶剂,-85~-65℃保存,有效期2年。产品对热、光敏感,建议分装后,低温干燥,避光保存,避免反复冻融。
Q:该试剂缓冲液是什么?配置成工作液后可以放置多久?
A:易溶于DMSO。建议分装后-20ºC 避光保存,避免反复冻存,至少可存放 6 个月。
[1] Lin DL, Yao HY, Jia LH, et al. Phospholipase D-derived phosphatidic acid promotes root hair development under phosphorus deficiency by suppressing vacuolar degradation of PIN-FORMED2. New Phytol. 2020;226(1):142-155. doi:10.1111/nph.16330(IF:7.299)
[2] Wu J, Ni Y, Yang Q, et al. Long-term arsenite exposure decreases autophagy by increased release of Nrf2 in transformed human keratinocytes. Sci Total Environ. 2020;734:139425. doi:10.1016/j.scitotenv.2020.139425(IF:6.551)