NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor[2].IC50 & Target: Glutathione S-transferase P1-1 (GSTP1-1);
Apoptosis;
AutophagyIn Vitro: NBDHEX (0.05-20 μM; 48 hours; H69 and H69AR cells) is cytotoxic toward cell lung cancer H69 and H69AR cells[2].
NBDHEX (0-5 μM; 24 hours; H69AR cells) treatment results in a dose-dependent apoptosis in the H69AR cell line[2].
NBDHEX (3 μM; 1-12 hours; H69AR cells) treatment increases the phosphorylation of JNK/c-Jun in H69AR cells in a time-dependent fashion[2].
NBDHEX treatment shows a marked increase in phosphorylation of p38MAPK, and also increases GSSG content in a time-dependent manner in H69 cells[2].In Vivo: NBDHEX (0.8-80 mg/kg/day; oral administration; daily; for 15 days; SCID female mice) treatment results a statistically significant tumour inhibition (approximately 70%)[2].