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Submit ReviewES 936
Description: Mechanism-based inhibitor of NAD(P)H:quinone oxidoreductase (NQO1)
Chemical Name: 5-Methoxy-1,2-dimethyl-3-[(4-nitrophenyoxy)methyl]-1H-indole
Purity: ≥98% (HPLC)
Biological Activity for ES 936
Mechanism-based inhibitor of NAD(P)H:quinone oxidoreductase (NQO1). Induces growth inhibition in human pancreatic carcinoma (MIA PaCa-2) and adenocarcinoma (BxPC-3) cell lines with IC50 values of 108 and 365 nM respectively. Also inhibits TNF-α-induced E-selectin protein expression in human bone marrow endothelial cells. Exhibits no effects on other cellular reductases or levels of acid-soluble thiols.
Technical Data for ES 936
| M. Wt | 356.33 |
| Formula | C18H16N2O6 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 192820-78-3 |
| Smiles | O=C(C=C1OC)C2=C(C(COC3=CC=C([N+]([O-])=O)C=C3)=C(C)N2C)C1=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for ES 936
References for ES 936
References are publications that support the biological activity of the product.
Dehn et al (2006) 5-Methoxy-1,2-dimethyl-3-[(4-nitrophenoxy)methyl]indole-4,7-dione, a mechanism-based inhibitor of NAD(P)H:quinone oxidoreductase 1, exhibits activity against human pancreatic cancer in vitro and in vivo. Mol.Cancer Ther. 5 1702 PMID: 16891456
Dehn et al (2003) Biochemical, cytotoxic, and genotoxic effects of ES936, a mechanism-based inhibitor of NAD(P)H:quinone oxidoreductase 1, in cellular systems. Mol.Pharmacol. 64 714 PMID: 12920209
Zhou et al (2010) NAD(P)H:quinone oxidoreductase 1-compromised human bone marrow endothelial cells exhibit decreased adhesion molecule expression and CD34 hematopoietic cell adhesion. J.Pharm.Exp.Ther. 334 260 PMID: 20378716
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Keywords: ES 936, ES 936 supplier, ES936, mechanism-based, inhibitor, NADPH, quinone, oxidoreductase, NQO1, inhibitors, inhibits, NADH, Other, Reductase, 4022, Tocris Bioscience
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