ES 936

ES 936 is a potent and specific NQO1 inhibitor. ES 936 inhibits the growth of MIA PaCa-2 and BxPC-3 cells, with IC₅₀ values of 108 nM and 365 nM, respectively. ES936 significantly inhitbits the growth rate of MIA PaCa-2 xenograft tumors in mice. ES 936 can be used for the study of pancreatic cancer^[1][2][3]. In Vitro:ES 936 (0-250 nM, 30-120 min) inhibits over 95% of NQO1 activity in HCT116, HT-29, MDA468 NQ16, MIA PaCa-2 and BxPC-3 cells^[1][2].
ES 936 (100 nM, 30 min pretreatment) increases the IC₅₀ of streptonigrin by ~6-fold in MDA468 NQ16 cells and ~2-fold in HCT116 cells, abrogating its toxicity^[1].
ES 936 (0-500 nM, 2 h) induces a dose-dependent increase in DNA strand breaks and stimulates low levels of NAD(P)H oxidation in rat liver microsomes^[1].
ES 936 (100 nM, 2 h pretreatment) significantly inhibits TNF-induced E-selectin expression and reduces TNF-induced VCAM-1 and ICAM-1 protein levels in transformed human bone marrow endothelial cells (TrHBMECs)^[3].
ES936 (100 nM, 2 h pretreatment) leads to a marked reduction in TNF-induced adhesion of CD34⁺ KG1a cells to TrHBMECs in a parallel plate flow chamber assay^[3].
In Vivo:ES936 (5 mg/kg, i.p., daily for 10 days) significantly inhibits the growth rate of MIA PaCa-2 xenograft tumors in female athymic nude mice^[2].