ES 936

SKU: orb1704542

Description

ES 936 is a potent and selective NQO1 inhibitor, achieving >95% enzyme inhibition at 100 nM within 30 minutes. Its cell line-dependent activity duration can induce limited DNA strand breaks, making it a valuable research tool for studying NQO1 function in cancer biology and oxidative stress response in vitro.

Research Area

Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 192820-78-3
• MW: 356.33
• Formula: C₁₈H₁₆N₂O₆
• SMILES: O=C1C=C(OC)C(=O)C2=C1N(C(=C2COC3=CC=C(C=C3)N(=O)=O)C)C
• Target: Others,NADPH,Reductase,NF-κB
• Solubility: DMSO:1 mg/mL (2.81 mM)

Bioactivity

• Target IC50:
  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|Streptonigrin cytotoxicity in MDA468 NQ-16 cells (with ES936 pretreatment):13 ± 0.4 nM |Streptonigrin cytotoxicity in HCT116 cells (with ES936 pretreatment):11 ± 0.6 nM|Cell proliferation (HCT116 cells):569 ± 48 nM
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• 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. 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ES 936, ES936, ES-936

Compound Identifiers

PubChem CID

4470790