WS-384 is an orally active dual inhibitor of LSD1 and DCN1-UBC12 protein-protein interactions, with IC50 values of 338.79 nM and 14.81 nM, respectively. It exhibits anticancer properties, causing cell cycle arrest, DNA damage, and inducing apoptosis (apoptosis). WS-384 can be applied in research on non-small cell lung cancer (NSCLC).

WS-384, at concentrations of 1-32 μM for 24-72 hours, effectively inhibits the growth of A549 and H1975 cells in a time- and dose-dependent manner, with an IC₅₀ ranging from 2.15 to 6.67 μM, demonstrating its anticancer properties. At 1-8 μM for 48 hours, WS-384 increases the expression levels of p21 gene and protein in A549 and H1975 cells by inhibiting the ubiquitin-like modification of cullin 1 and reducing H3K4 demethylation at the CDKN1A promoter, leading to G2/M cell cycle arrest and apoptosis. Additionally, WS-384 (1-8 μM; 48 h) can cause DNA damage.

WS-384, administered orally at a dose of 25-50 mg/kg once daily for 36 days, effectively inhibits the growth of NSCLC tumors in a xenograft model using BALB/c nude mice, while maintaining low toxicity.