FTase-IN-1

FTase-IN-1 (compound 17a) is a potent and specific inhibitor of fanesyl transferase (FTase) with an IC50 of 0.35 μM. FTase-IN-1 displays cytotoxicity potential and antitumor activity[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Farnesyl Transferase

IC50: 0.35 μM (fanesyl transferase)[1]

FTase-IN-1 (compound 17a) (10 μM, 48 h) is an inhibitors of farnesyl transferase (FTase) and inhibits NCI-60 cells proliferation in vitro[1]. FTase-IN-1 (10 μM, 48 h) arrests the cell growth of multiple cancer cell lines with GI50 range from 1.8 to 6.5 nM[1]. Cell Viability Assay[1] Cell Line: NCI-H522 (lung cancer), COLO-205 and HT29 (colon cancer), SF-539 (human glioblastoma), MDA-MB-435 (melanoma), OVCAR-3 (ovarian cancer) and A498 (renal cancer) Concentration: 10 μM Incubation Time: 48 hours Result: Inhibited cell growth and showed strong antitumor activity.

[1]. Iuliana-Monica Moise, et al. Indolizine-phenothiazine hybrids as the first dual inhibitors of tubulin polymerization and farnesyltransferase with synergistic antitumor activity. Bioorg Chem. 2020 Oct; 103: 104184.