Cat. No.: HY-19357

Erenapurstat

(Synonyms: E3330; APX-3330)

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

Erenapursta (E3330) is a direct, orally active and selective inhibitor of Ape-1 (apurinic/apyrimidinic endonuclease 1)/Ref-1 (redox factor-1) redox. Erenapursta is able to impair tumor growth and blocks the activity of NF-κB, AP-1, and HIF-1α in pancreatic cancer. Erenapursta shows anticancer activities.

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Pureté: 99.67%
CAS No.: 136164-66-4
Formule: C₂₁H₃₀O₆
Masse moléculaire:378.46

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Erenapurstat Chemical Structure

CAS No.: 136164-66-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (4)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

Ape-1, Ref-1^[1]

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis :

Voir tous les produits spécifiques à Isoform NF-κB :

Voir tous les produits spécifiques à Isoform AP-1 :

Voir tous les produits spécifiques à Isoform HIF/HIF Prolyl-Hydroxylase :

Voir tous les produits spécifiques à Isoform VEGFR :

In Vitro

Erenapursta (E3330) (0-50 μM, 48 h) inhibits the growth of HUVECs, PCECs and EPCs^[1].
Erenapursta (0-5 μM) reduces secreted and intracellular VEGF (vascular endothelial growth factor) expression by pancreatic cancer cells, while concomitantly downregulating the cognate receptor Flk-1/KDR on PCECs^[1].
Erenapursta (0-1 μM) inhibits the differentiation of bone marrow mesenchymal stem cells (BM-MSCs) into CD31⁺ cells of endothelial lineage^[1].
Erenapursta (0-50 μM, 72 h) decreases cell viability in H1975 cells about 45% at 50 μM^[2].
Erenapursta (0-30 μM) inhibits the growth and migration of pancreatic cancer cells^[3].
Erenapursta (0-30 μM) significantly enhances intracellular ROS level and inhibits CD44 expression in PANC1 cells^[3].

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

Cell Proliferation Assay^[1]

Cell Line:

Human umbilical vein endothelial cells (HUVECs), murine pancreatic cancer associated endothelial cells (mPCECs), human endothelial progenitor cells (hEPCs)
Concentration:

1, 5, and 10 μM (HUVECs); 1. 5, 10. 20. 30, 40, and 50 μM (mPCECs); 1, 5, 10, 15, 20, 25, and 30 μM (hEPCs)
Incubation Time:

48 h
Result:

Inhibited the growth of HUVECs, PCECs and EPCs.

Western Blot Analysis^[1]

Cell Line:

mPCECs
Concentration:

1, 5, and 10 μM
Incubation Time:

48 h
Result:

Inhibited the growth of HUVECs, PCECs and EPCs.

Cell Viability Assay^[2]

Cell Line:

H1975 cells
Concentration:

0, 5, 10, 20, 30, 40, and 50 μM
Incubation Time:

72 h
Result:

Showed decreased cell viability in about 45% at 50 µM.

In Vivo

Erenapursta (E3330) (25 mg/kg, Orally, 5 daily, five days each week for three weeks) is neuroprotective against cisplatin-induced alterations in capsaicin-induced vasodilation^[4].
Erenapursta (0-100 mg/kg, Orally, once) attenuates the liver injury when given at 1 h, 6 h or 12 h after galactosamine challenge^[5].

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

Animal Model:

Sprague-Dawley rats (adult male, 150-175 g)^[4]
Dosage:

25 mg/kg
Administration:

Orally, 5 daily, five days each week for three weeks
Result:

Attenuated the cisplatin-induced decrease in capsaicin-induced vasodilatation in the rat hindpaw.

Animal Model:

Male Fischer (F344/DuCrj) rats (160-190 g)^[5]
Dosage:

0, 10, 30, and 100 mg/kg
Administration:

Orally, 1 h, 6 h or 12 h after galactosamine challenge
Result:

Attenuated the liver injury when given at 1 h, 6 h or 12 h after galactosamine challenge.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 136164-66-4
Appearance Solid
Masse moléculaire 378.46
Formule C₂₁H₃₀O₆
Color Yellow to orange
SMILES

CCCCCCCCC/C(C(O)=O)=C\C1=C(C)C(C(OC)=C(OC)C1=O)=O
Synonyms

E3330; APX-3330
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Journal Impact Factor

Cell Death Dis

Cephalomannine inhibits hypoxia-induced cellular function via the suppression of APEX1/HIF-1α interaction in lung cancer. [Abstract]

2021 May 14;12(5):490. PMID: 33990544
J Allergy Clin Immunol

Role of APE1 redox function in chronic rhinosinusitis pathogenesis: Implications for targeted therapy. [Abstract]

2025 Jul 17:S0091-6749(25)00775-4. PMID: 40683569
Brain Behav Immun

Schwann cell-derived CXCL2 contributes to cancer pain by modulating macrophage infiltration in a mouse breast cancer model. [Abstract]

2023 Mar:109:308-320. PMID: 36754246
Int Immunopharmacol

Inhibitors of APE1 redox and ATM synergistically sensitize osteosarcoma cells to ionizing radiation by inducing ferroptosis. [Abstract]

2024 Sep 30:139:112672. PMID: 39032469

Solvant et solubilité

In Vitro:

DMSO : 120 mg/mL (317.07 mM; Need ultrasonic; 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

2.6423 mL

13.2114 mL

26.4229 mL

5 mM

0.5285 mL

2.6423 mL

5.2846 mL

10 mM

0.2642 mL

1.3211 mL

2.6423 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (5.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (536 KB)
- English - EN (536 KB)
- Français - FR (536 KB)
- Deutsch - DE (536 KB)
- Norwegian - NO (536 KB)
- Español - ES (536 KB)
- Swedish - SV (536 KB)
- Italian - IT (536 KB)
- Korean - KR (536 KB)
- Portuguese - PT (536 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)
Instruction de manipulation (2659 KB)

Références

[1]. Zou GM, et al. The Ape-1/Ref-1 redox antagonist E3330 inhibits the growth of tumor endothelium and endothelial progenitor cells: therapeutic implications in tumor angiogenesis. J Cell Physiol. 2009 Apr;219(1):209-18. [Content Brief]

[2]. Manguinhas R, et al. Impact of the APE1 Redox Function Inhibitor E3330 in Non-small Cell Lung Cancer Cells Exposed to Cisplatin: Increased Cytotoxicity and Impairment of Cell Migration and Invasion. Antioxidants (Basel). 2020 Jun 24;9(6):550. [Content Brief]

[3]. Zou GM, et al. Small-molecule inhibitor of the AP endonuclease 1/REF-1 E3330 inhibits pancreatic cancer cell growth and migration. Mol Cancer Ther. 2008 Jul;7(7):2012-21. [Content Brief]

[4]. Kelley MR, et al. Role of the DNA base excision repair protein, APE1 in cisplatin, oxaliplatin, or carboplatin induced sensory neuropathy. PLoS One. 2014 Sep 4;9(9):e106485. [Content Brief]

[5]. Nagakawa J, et al. Protective effect of E3330, a novel quinone derivative, in galactosamine-induced hepatitis in rats. J Pharmacol Exp Ther. 1993 Jan;264(1):496-500. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6423 mL	13.2114 mL	26.4229 mL	66.0572 mL
	5 mM	0.5285 mL	2.6423 mL	5.2846 mL	13.2114 mL
	10 mM	0.2642 mL	1.3211 mL	2.6423 mL	6.6057 mL
	15 mM	0.1762 mL	0.8808 mL	1.7615 mL	4.4038 mL
	20 mM	0.1321 mL	0.6606 mL	1.3211 mL	3.3029 mL
	25 mM	0.1057 mL	0.5285 mL	1.0569 mL	2.6423 mL
	30 mM	0.0881 mL	0.4404 mL	0.8808 mL	2.2019 mL
	40 mM	0.0661 mL	0.3303 mL	0.6606 mL	1.6514 mL
	50 mM	0.0528 mL	0.2642 mL	0.5285 mL	1.3211 mL
	60 mM	0.0440 mL	0.2202 mL	0.4404 mL	1.1010 mL
	80 mM	0.0330 mL	0.1651 mL	0.3303 mL	0.8257 mL
	100 mM	0.0264 mL	0.1321 mL	0.2642 mL	0.6606 mL

Erenapurstat

4 Cited Publications

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Erenapurstat

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Erenapurstat

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis

Voir tous les produits spécifiques à Isoform NF-κB

Voir tous les produits spécifiques à Isoform AP-1

Voir tous les produits spécifiques à Isoform HIF/HIF Prolyl-Hydroxylase

Voir tous les produits spécifiques à Isoform VEGFR

Activité biologique

Chemical Information

Publications (4)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Erenapurstat Related Classifications

HY-19357 Related Classifications