ES 936

Discontinued Product

Unfortunately ES 936 (Cat. No. 4022) has been withdrawn from sale for commercial reasons.
Cat.No. 4022 - ES 936 | C18H16N2O6 | CAS No. 192820-78-3
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)
Datasheet
Citations
Literature

Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

Preparing Stock Solutions

The following data is based on the product molecular weight 356.33. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.81 mL 14.03 mL 28.06 mL
5 mM 0.56 mL 2.81 mL 5.61 mL
10 mM 0.28 mL 1.4 mL 2.81 mL
50 mM 0.06 mL 0.28 mL 0.56 mL

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Product Datasheets

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References

References are publications that support the products' biological activity.

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, supplier, ES936, mechanism-based, inhibitor, NADPH, quinone, oxidoreductase, NQO1, inhibitors, inhibits, NADH, oxidoreductase, Other, Reductase, Other, Reductase, Tocris Bioscience

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