GRP78-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GRP78-IN-1 

GRP78-IN-1 与 GRP78 残基具有多种相互作用，结合能为 -8.07 kcal/mol。GRP78-IN-1 在癌细胞中显示出有效的细胞毒性、抗增殖作用。GRP78-IN-1 在乳腺癌细胞中表现出有前景的凋亡和伤口愈合特性。

GRP78-IN-1

GRP78-IN-1 Chemical Structure

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生物活性

GRP78-IN-1 exhibits several interactions with GRP78 residues with binding energy of -8.07 kcal/mol. GRP78-IN-1 shows the potent cytotoxic, anti-proliferative in cancer cells. GRP78-IN-1 exhibits promising apoptosis in breast cancer cells and wound healing properties[1].

IC50 & Target

Grp78

 

体外研究
(In Vitro)

GRP78-IN-1 (compound 3i) (0.01, 0.1, 1, 10, 100 µM; 48 h) shows the most potent cytotoxic effect (IC50s of 2.06, 12.57, 9, 18, 4.9, 2.19, 62.48 µM in MCF-1, PANC-1, HCT-116, PC-3, A549, MDA-MB-231 and FR-2 cells, respectively)[1].
GRP78-IN-1 (1, 2, 4, 6 µM) shows a steady increase in the expression of pro-apoptotic proteins viz. Par-4, apoptotic cascade in BAX and cleaved caspase 9 cells[1].
GRP78-IN-1 (1, 2, 4, 6 µM; 48 h) inhibits the motility of MCF-7 and A549 cells in a dose-dependent manner[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: MCF-1, MDA-MB-231, PANC-1, HCT-116, PC-3, A549, FR-2cells
Concentration: 0.01, 0.1, 1, 10, 100 µM
Incubation Time: 48 h
Result: Showed the most promising cytotoxic effect (IC50s is 2.06, 12.57, 9, 18, 4.9, 2.19, 62.48 µM in MCF-1, PANC-1, HCT-116, PC-3, A549, MDA-MB-231 and FR-2 cells, respectively).

Western Blot Analysis[1]

Cell Line: BCL-2, BAX, cleaved caspase 9, MCF-7, A549 cells
Concentration: 1, 2, 4, 6 µM
Incubation Time:
Result: Showed a steady increase in the expression of pro-apoptotic proteins viz. Par-4, apoptotic cascade in BAX and cleaved caspase 9 cells.

分子量

342.40

Formula

C21H23FO3
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]. Rasool JU, et al. Palladium catalyzed migratory heck coupling of arteannuin B and boronic acids: An approach towards the synthesis of antiproliferative agents in breast and lung cancer cells. Bioorg Chem. 2022, 122:105694.

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