RIP1/RIP3/MLKL activator 1

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RIP1/RIP3/MLKL activator 1 

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。

RIP1/RIP3/MLKL activator 1

RIP1/RIP3/MLKL activator 1 Chemical Structure

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生物活性

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[1].

IC50 & Target

RIP1, RIP3, MLKL[1]
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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC50 values 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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

676.93

Formula

C43H56N4O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

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