RIP1/RIP3/MLKL activator 1|cas:2682850-41-3|西域试剂

RIP1/RIP3/MLKL activator 1,97.0%

产品编号：Bellancom-144828| CAS NO：2682850-41-3| 分子式：C₄₃H₅₆N₄O₃| 分子量：676.93

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货号	价格	库存与货期
Bellancom-144828	￥3500.00	杭州北京（现货）
Bellancom-144828	￥5800.00	杭州北京（现货）
Bellancom-144828	￥11000.00	杭州北京（现货）

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RIP1/RIP3/MLKL activator 1

产品介绍

RIP1/RIP3/MLKL activator 1 (Compound 6i) 是一种有效的抗胶质瘤 (anti-glioma) 活性分子。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 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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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

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.

西域 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)
Dosage:	2.50 ng/tail
Administration:	Microinjection; 48 h
Result:	Remarkably reduced the U251 xenografts fluorescence intensity.

体内研究

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.

西域 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)
Dosage:	2.50 ng/tail
Administration:	Microinjection; 48 h
Result:	Remarkably reduced the U251 xenografts fluorescence intensity.

体内研究

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.

西域 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)
Dosage:	2.50 ng/tail
Administration:	Microinjection; 48 h
Result:	Remarkably reduced the U251 xenografts fluorescence intensity.