RIP1/RIP3/MLKL activator 1 (Compound 6i) 是一种有效的抗胶质瘤 (anti-glioma) 药物。RIP1/RIP3/MLKL activator 1 通过激活RIP1/RIP3/MLKL通路诱导细胞坏死 （necroptosis）。 RIP1/RIP3/MLKL activator 1 可透过血脑屏障。
| 生物活性 | RIP1/RIP3/MLKL activator 1 (Compound 6i) is a potentanti-gliomaagent. RIP1/RIP3/MLKL activator 1 inducesnecroptosisthroughRIP1/RIP3/MLKLpathway. RIP1/RIP3/MLKL activator 1 exerts acceptable BBB permeability[1]. |
| IC50& Target | |
体外研究
(In Vitro) | RIP1/RIP3/MLKL activator 1 (Compound 6i) (96 h) shows antiproliferative activities in human glioma cell lines[1].
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[1].
RIP1/RIP3/MLKL activator 1 (10 μM, 0-72 h) shows acceptable stability[1].
RIP1/RIP3/MLKL activator 1 (0-2 μM, 24 h) effectively inhibits the migration of U251 cells[1].
RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway, and induces mitochondrial depolarization in U251 cells[1].
RIP1/RIP3/MLKL activator 1 could not induce apoptosis in U251 cells[1].
Cell Proliferation Assay[1] | Cell Line: | A172, LN229, U87, U251 and L02 cell lines | | Concentration: | 0-4 μM for U251 cells | | Incubation Time: | 96 h; 24, 48, and 72 h for U251 cells | | Result: | Showed antiproliferative activity with IC50values of 3.03 ± 0.70, 1.78 ± 0.79, 1.22 ± 0.89, 0.94 ± 0.45, and 0.99 ± 0.46 μM against A172, LN229, U87, U251 and L02 cells, respectively. Time- and concentration-dependently inhibited the growth in U251 cells. |
Western Blot Analysis[1] | Cell Line: | U251 | | Concentration: | 0, 0.5, 1, 2, and 4 μM | | Incubation Time: | 24 or 48 h | | Result: | Concentration-dependently upregulated the expression of p-RIP1, RIP1, p-RIP3, RIP3, p-MLKL, and MLKL at 24 or 48 h. |
|
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[1].
| Animal Model: | Zebrafish wide-type AB strain; 200 CM-DiI labeled U251 cells were transplanted into yolk sac of each wild-type zebrafish embryos at 2 dpf (2 days postfertilization)[1] | | Dosage: | 2.50 ng/tail | | Administration: | Microinjection; 48 h | | Result: | Remarkably reduced the U251 xenografts fluorescence intensity. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 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) |
m.cnreagent.com