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 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].

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.

C21H23FO3

342.4

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years