Drug intelligence / Profile preview

ES-936

Development stage
Preclinical
Modality
Small Molecules
01

Overview

ES-936 is a potent and specific small molecule inhibitor of NAD(P)H:quinone oxidoreductase 1 (NQO1), also known as NAD(P)H dehydrogenase [quinone] 1. It acts as a mechanism-based (irreversible) inhibitor, effectively blocking NQO1 activity at nanomolar concentrations—over a thousand times more potent than the non-specific inhibitor dicoumarol. In cellular systems, ES‑936 rapidly inhibits more than 95% of NQO1 activity within minutes and is stable in media for at least two hours. Its inhibition is highly selective for NQO1 with no significant effects on other cellular reductases or acid-soluble thiols. Preclinical studies show that it induces growth inhibition in certain human cancer cell lines (e.g., pancreatic carcinoma MIA PaCa‑2 and adenocarcinoma BxPC‑3). It has also been used to study the role of NQO1 in drug metabolism and cytotoxicity[2][3][5].

Other names
1H-Indole-4,7-dione, 5-methoxy-1,2-dimethyl-3-[(4-nitrophenoxy)methyl]-UNII-1XI90I177MUNII1XI90I177MUNII 1XI90I177MCAS 192820-78-3CAS192820-78-3CAS-192820-78-3
02

Targets

NQO1

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