Art. -Nr.: HY-100367

ES 936

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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.

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Reinheit: 98.66%
CAS. Nr.: 192820-78-3
Formel: C₁₈H₁₆N₂O₆
Molecular Weight:356.33

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

ES 936 Chemical Structure

CAS. Nr.: 192820-78-3

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle NF-κB Isoform-spezifische Produkte anzeigen :

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]
NCI-H460	IC₅₀	2.81 μM Compound: 5u	Cytotoxicity was measured on non-small cell lung cancer(NSCLC) in H460 cell lines. Cytotoxicity was measured on non-small cell lung cancer(NSCLC) in H460 cell lines.	[PMID: 9822546]
NCI-H596	IC₅₀	2 μM Compound: 5u	Cytotoxicity was measured on non-small cell lung cancer(NSCLC) in H596 cell lines. Cytotoxicity was measured on non-small cell lung cancer(NSCLC) in H596 cell lines.	[PMID: 9822546]

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.

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).

Chemical Information

CAS. Nr. 192820-78-3
Appearance Solid
Molecular Weight 356.33
Formel C₁₈H₁₆N₂O₆
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Cell Death Differ

A neutrophil-intrinsic CKLF1-PKM2 axis drives glycolytic flux for de novo DAG synthesis and pro-inflammatory ROS production. [Abstract]

2026 May 12. PMID: 42120940

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8064 mL

14.0319 mL

28.0639 mL

5 mM

0.5613 mL

2.8064 mL

5.6128 mL

10 mM

---

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 2.5 mg/mL (7.02 mM); Suspended solution; Need ultrasonic

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Dehn DL, et al. Biochemical, cytotoxic, and genotoxic effects of ES936, a mechanism-based inhibitor of NAD(P)H:quinone oxidoreductase 1, in cellular systems. Mol Pharmacol. 2003 Sep;64(3):714-20. [Content Brief]

[2]. Dehn DL, et al. 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. [Content Brief]

[3]. Zhou H, et al. NAD(P)H:quinone oxidoreductase 1-compromised human bone marrow endothelial cells exhibit decreased adhesion molecule expression and CD34+ hematopoietic cell adhesion. J Pharmacol Exp Ther. 2010 Jul;334(1):260-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
DMSO	5 mM	0.5613 mL	2.8064 mL	5.6128 mL	14.0319 mL

Keywords

ES 936

1 Cited Publications

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ES 936

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Publications Citing Use of MedChemExpress (MCE) ES 936

Alle NF-κB Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ES 936 Related Classifications

HY-100367 Related Classifications