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].

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.