RIP1/RIP3/MLKL activator 1 (Compound 6i) is a potent anti-glioma agent. RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway. RIP1/RIP3/MLKL activator 1 exerts acceptable BBB permeability.
性状
Solid
IC50 & Target[1][2]
RIP1, RIP3, MLKL
体外研究(In Vitro)
RIP1/RIP3/MLKL activator 1 (Compound 6i) (96 h) shows antiproliferative activities in human glioma cell lines.RIP1/RIP3/MLKL activator 1 (0-4 μM, 0-72 h) exhibits remarkable antiproliferative activity for U251 cells in a time- and concentration-dependent manner.RIP1/RIP3/MLKL activator 1 (10 μM, 0-72 h) shows acceptable stability.RIP1/RIP3/MLKL activator 1 (0-2 μM, 24 h) effectively inhibits the migration of U251 cells.RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway, and induces mitochondrial depolarization in U251 cells.RIP1/RIP3/MLKL activator 1 could not induce apoptosis in U251 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
RIP1/RIP3/MLKL activator 1 (Compound 6i) (2.50 ng/tail; i.v.; 48 h) inhibits U251 cell proliferation in vivo and exerts acceptable BBB permeability. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Yao Feng, et al. Synthesis and biological evaluation of celastrol derivatives as potential anti-glioma agents by activating RIP1/RIP3/MLKL pathway to induce necroptosis. Eur J Med Chem. 2022 Feb 5;229:114070.