c-Met/HDAC-IN-3

c-Met/HDAC-IN-3 (Compound 15f) is a dual c-Met and HDAC inhibitor with IC50 values of 12.50 nM and 26.97 nM against c-Met and HDAC1, respectively. c-Met/HDAC-IN-3 induces apoptosis and cause cell cycle arrest in G2/M phase[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC

Signaling Pathways >> Epigenetics >> HDAC

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR

c-Met:12.50 nM (IC50)

HDAC1:26.97 nM (IC50)

c-Met/HDAC-IN-3 (Compound 15f) (0-20 μM, 72 h) shows antiproliferative activities against HCT-116, MCF-7 and A549 cells[1]. c-Met/HDAC-IN-3 (0-5 μM, 48 h) induces apoptosis and arrests cell cycle at G2/M phase[1]. Cell Proliferation Assay[1] Cell Line: HCT-116, MCF-7 and A549 Concentration: 0-20 µM Incubation Time: 72 h Result: Showed antiproliferative activities with IC50 values of 0.54 ± 0.05, 0.28 ± 0.02 and 1.08 ± 0.44 μM against HCT-116, MCF-7 and A549 cells. Apoptosis Analysis[1] Cell Line: HCT-116 Concentration: 0.2, 1.0 and 5.0 µM Incubation Time: 48 h Result: Resulted in 6.97%, 7.08% and 13.21% cells apoptosis at 0.2, 1.0 and 5.0 µM, respectively. Cell Cycle Analysis[1] Cell Line: HCT-116 Concentration: 0.2, 1.0 and 5.0 µM Incubation Time: 48 h Result: Showed an obvious increase in the proportion of cells in G2/M phase in a dose-dependent manner.

[1]. Hu H, et al. Discovery of novel dual c-Met/HDAC inhibitors as a promising strategy for cancer therapy. Bioorg Chem. 2020 Aug;101:103970.