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ES 936 is a potent and selective NQO1 inhibitor, inhibiting more than 95% of NQO1 activity within 30 minutes at a concentration of 100 nM, with a cell line-dependent inhibition duration resulting in a small number of DNA strand breaks.
Pack Size | Price | Availability | Quantity |
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1 mg | $70 | In Stock |
Description | ES 936 is a potent and selective NQO1 inhibitor, inhibiting more than 95% of NQO1 activity within 30 minutes at a concentration of 100 nM, with a cell line-dependent inhibition duration resulting in a small number of DNA strand breaks. |
Targets&IC50 | Streptonigrin cytotoxicity in HCT116 cells (with ES936 pretreatment):11 ± 0.6 nM, Streptonigrin cytotoxicity in HCT116 cells (without ES936 pretreatment):6.7 ± 1 nM, Cell proliferation (reflecting cytotoxicity) in MDA468 NQ-16 cells:732 ± 49 nM, Streptonigrin cytotoxicity in MDA468 NQ-16 cells (without ES936 pretreatment):2.2 ± 0.06 nM, Cell proliferation in HCT116 cells:569 ± 48 nM, Streptonigrin cytotoxicity in MDA468 NQ-16 cells (with ES936 pretreatment):13 ± 0.4 nM |
In vitro | ES 936 exhibited relatively low cytotoxicity toward MDA468 NQ-16 (high NQO1 activity) and HCT116 (low NQO1 activity) cells, with IC₅₀ values of 732 ± 49 nM and 569 ± 48 nM, respectively. These concentrations are approximately 8–20 times higher than those required for effective NQO1 inhibition, indicating weak intrinsic growth-inhibitory activity.[1] In co-treatment experiments, ES 936 pretreatment significantly increased the IC₅₀ of streptonigrin, from 2.2 ± 0.06 nM to 13 ± 0.4 nM in MDA468 NQ-16 cells (approximately 6-fold), and from 6.7 ± 1 nM to 11 ± 0.6 nM in HCT116 cells (approximately 2-fold). These results indicate that ES 936 reduces the bioactivation and cytotoxicity of streptonigrin by inhibiting NQO1 activity.[1] |
Alias | ES936 |
Molecular Weight | 356.33 |
Formula | C18H16N2O6 |
Cas No. | 192820-78-3 |
Smiles | O=C1C=C(OC)C(=O)C2=C1N(C(=C2COC3=CC=C(C=C3)N(=O)=O)C)C |
Relative Density. | 1.38 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||
Solubility Information | DMSO: 1 mg/mL (2.81 mM), Sonication is recommended. | ||||||||||
Solution Preparation Table | |||||||||||
DMSO
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