化合物 GRP78-IN-1 T61106

Product Introduction
Bioactivity


英文名: GRP78-IN-1

描述: GRP78-IN-1 displays interactions with specific residues on the GRP78 protein with a binding energy of -8.07 kcal/mol. This compound possesses potent cytotoxic and anti-proliferative effects on cancer cells, particularly demonstrating promising apoptosis in breast cancer cells and wound healing properties [1].

体外活性: GRP78-IN-1 (compound 3i) (0.01, 0.1, 1, 10, 100 μM; 48 h) shows the most potent cytotoxic effect (IC 50 s 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]. 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 (IC 50 s 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途