2. Metabolic Enzyme/Protease NF-κB
  3. Quinone Reductase NF-κB
  4. ES 936

ES 936 is a potent and specific NQO1 inhibitor. ES 936 inhibits the growth of MIA PaCa-2 and BxPC-3 cells, with IC50 values of 108 nM and 365 nM, respectively. ES936 significantly inhitbits the growth rate of MIA PaCa-2 xenograft tumors in mice. ES 936 can be used for the study of pancreatic cancer.

For research use only. We do not sell to patients.

ES 936

ES 936 Chemical Structure

CAS No. : 192820-78-3

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Based on 1 publication(s) in Google Scholar

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Description

ES 936 is a potent and specific NQO1 inhibitor. ES 936 inhibits the growth of MIA PaCa-2 and BxPC-3 cells, with IC50 values of 108 nM and 365 nM, respectively. ES936 significantly inhitbits the growth rate of MIA PaCa-2 xenograft tumors in mice. ES 936 can be used for the study of pancreatic cancer[1][2][3].

Cellular Effect
Cell Line Type Value Description References
MIA PaCa-2 IC50
508 nM
Compound: 1, ES936
Cytotoxicity against human MIA PaCa2 cells after 72 hrs by MTT assay
Cytotoxicity against human MIA PaCa2 cells after 72 hrs by MTT assay
[PMID: 17944451]
MIA PaCa-2 IC50
629 nM
Compound: 1, ES936
Cytotoxicity against human MIA PaCa2 cells after 4 hrs by MTT assay
Cytotoxicity against human MIA PaCa2 cells after 4 hrs by MTT assay
[PMID: 17944451]
In Vitro

ES 936 (0-250 nM, 30-120 min) inhibits over 95% of NQO1 activity in HCT116, HT-29, MDA468 NQ16, MIA PaCa-2 and BxPC-3 cells[1][2].
ES 936 (100 nM, 30 min pretreatment) increases the IC50 of streptonigrin by ~6-fold in MDA468 NQ16 cells and ~2-fold in HCT116 cells, abrogating its toxicity[1].
ES 936 (0-500 nM, 2 h) induces a dose-dependent increase in DNA strand breaks and stimulates low levels of NAD(P)H oxidation in rat liver microsomes[1].
ES 936 (100 nM, 2 h pretreatment) significantly inhibits TNF-induced E-selectin expression and reduces TNF-induced VCAM-1 and ICAM-1 protein levels in transformed human bone marrow endothelial cells (TrHBMECs)[3].
ES936 (100 nM, 2 h pretreatment) leads to a marked reduction in TNF-induced adhesion of CD34+ KG1a cells to TrHBMECs in a parallel plate flow chamber assay[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ES 936 Related Antibodies

Cell Viability Assay[3]

Cell Line: Transformed human bone marrow endothelial cells (TrHBMECs)
Concentration: 100 nM
Incubation Time: 2 h pretreatment
Result: Decreased TNF-stimulated E-selectin protein levels.
Reduced TNF-induced VCAM-1 and ICAM-1 protein levels.
Resulted in lower nuclear levels of phospho-p65, phospho-c-Jun, and phospho-ATF2 in TrHBMECs.
In Vivo

ES936 (5 mg/kg, i.p., daily for 10 days) significantly inhibits the growth rate of MIA PaCa-2 xenograft tumors in female athymic nude mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MIA PaCa-2 cells in log-phase growth (2×106 in 100 µL of 75:25 unsupplemented medium/Matrigel) were subcutaneously injected into the right flanks of 5- to 6-week-old female athymic nude mice (Ncr nu/nu)[2]
Dosage: 5 mg/kg
Administration: i.p. daily for 10 days
Result: Achieved a maximal T/C value of 47% based on tumor volume analysis in MIA PaCa-2 xenograft tumors.
Showed no obvious toxicities and no difference in body weight between ES936-treated and control (DMSO) animals.
Significantly slowed the growth rate of MIA PaCa-2 xenograft tumors, with the inhibitory effect more significant during treatment (days 1-10) than after cessation of therapy (days 11-20).
Molecular Weight

356.33

Formula

C18H16N2O6
CAS No.
Appearance

Solid

Color

Orange to red

SMILES

O=C(C(OC)=C1)C2=C(N(C)C(C)=C2COC3=CC=C([N+]([O-])=O)C=C3)C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (5.61 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8064 mL 14.0319 mL 28.0639 mL
5 mM 0.5613 mL 2.8064 mL 5.6128 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8064 mL 14.0319 mL 28.0639 mL 70.1597 mL
5 mM 0.5613 mL 2.8064 mL 5.6128 mL 14.0319 mL
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ES 936 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ES 936192820-78-3ES936ES-936Quinone ReductaseNF-κBNuclear factor-κBNuclear factor-kappaBNQO1specific inhibitorreactive oxygen speciesDicoumarolInhibitorinhibitorinhibit

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