Drug intelligence / Profile preview

alpha-phenylethyl isothiocyanate

Development stage
Preclinical
Lead developer
National Cancer Institute
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Alpha-phenylethyl isothiocyanate (α-PEITC) is a natural isothiocyanate compound investigated for its potent anti-tumor properties, particularly in malignant melanoma. It functions by depleting cellular glutathione (GSH) levels, thereby disabling the antioxidant defense system and inducing an aberrant accumulation of reactive oxygen species (ROS). This oxidative stress triggers apoptosis in cancer cells. Research indicates that α-PEITC is effective against melanoma cells resistant to standard therapies like vemurafenib and can act synergistically with alkylating agents such as carmustine and temozolomide. It has shown selectivity for malignant cells, with minimal sensitivity observed in normal melanocytes.

Other names
1-phenylethyl isothiocyanatealpha-PEITCα-phenylethyl isothiocyanate
02

Targets

MEKMRC (Mitochondrial respiratory chain proteins)GSTA1 (Glutathione S-transferase A1)Cyp (Cyclophilin family)KEAP1 (Kelch-like ECH-associated protein 1)GSTP1 (Glutathione S-transferase P)

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