Phenylethyl isothiocyanate demonstrates a broad spectrum of bioactivities and potential therapeutic applications. It acts as an inhibitor against various cancer cell lines, including human leukemia 60 cells (GC50: 0.84 µM, TC50: 1.37 µM), A549, T47D, MCF7, LoVo, MDA-MB-231, PC-3, Caco-2, UACC-903, HT1080, LS 174T, and OVCAR-3, showing varying IC50 values. It inhibits cell growth in MEF cells (IC50: 8000.0 nM for TSC2-deficient, 4700.0 nM for wild type), induces cell cycle arrest, and reduces glutathione levels in A549 cells. Phenylethyl isothiocyanate also exhibits notable antitumor activity, reducing tumor size by 40% in UACC-903 cells xenografted in mice.
Beyond its antiproliferative effects, Phenylethyl isothiocyanate has significant bioactivity in inhibiting human liver OATP transporters, TRPA1 (EC50: 370.0 nM), and TRPV1 channels, with an EC50 value indicating moderate activation. It also modulates MRP2-mediated transport, shows cytotoxic effects against nematodes (LC50: 4.15 µg/mL), and demonstrates fungistatic and fungitoxic properties against Sclerotinia sclerotiorum.
Additionally, it acts as a mechanism-based inhibitor of human CYP2E1 (Ki: 9980.0 nM) and shows mixed inhibition of CYP2A6 (Ki: 1700.0 nM) and CYP2A13 (Ki: 3800.0 nM). Increasing daunomycin accumulation in PANC-1 cells when combined with phenylhexyl isothiocyanate, Phenylethyl isothiocyanate also inhibits the activity of macrophage migration inhibitory factor, both in human cells and recombinant forms, and suppresses Serine/threonine-protein kinase mTOR complex 1-mediated HIF1alpha RNA translation (IC50: 7500.0 nM). Lastly, it demonstrates inhibition of USP9x with a notable association constant, indicating its potential as a multipurpose compound..
Note: Summary generated by AI. Data source: ChEMBL 