FAK-IN-5

FAK-IN-5 (Compound 8l) is a FAK signaling inhibitor. FAK-IN-5 induces cell apoptosis and autophagy[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FAK

Signaling Pathways >> Autophagy >> Autophagy

FAK-IN-5 (Compound 8l) (0-50 µM, 72 h) shows antiproliferative activity against cancer cells[1]. FAK-IN-5 (Compound 8l) causes cell detachment[1]. FAK-IN-5 (Compound 8l) (0-25 µM, 24 h) induces autophagy and apoptosis in HCT-116 cells[1]. Cell Proliferation Assay[1] Cell Line: K562, CEM, G361, MCF-7 and HCT-116 Concentration: 0-50 µM Incubation Time: 72 h Result: Showed antiproliferative activity with IC50 values of 6.3, 7.9, 6.3, 5.5 and 5.3 µM against K562, CEM, G361, MCF-7 and HCT-116 cells, respectively. Western Blot Analysis[1] Cell Line: HCT-116 Concentration: 1.25, 2.5, 5, 7, 10, 11, 17 and 25 µM Incubation Time: 1, 3, 5, 7 and 24 h Result: Caused the dephosphorylation of FAK, p130Cas and paxillin in a dose-dependent manner. The dephosphorylation of FAK at Y397 was observed at a much earlier time point. Detected the fragments of activated caspase-7 as well as the dose-dependent cleavage of poly (ADP-ribose) polymerase (PARP).

[1]. Jorda R, et al. Novel modified leucine and phenylalanine dipeptides modulate viability and attachment of cancer cells. Eur J Med Chem. 2020 Feb 15;188:112036.