Art. -Nr.: HY-14761

Bentamapimod

(Synonyms: AS 602801)

12 Cited Publications

Kundenbewertung

Based on 12 publication(s) in Google Scholar

Bentamapimod (AS 602801) is an ATP-competitive JNK inhibitor with IC₅₀ of 80 nM, 90 nM, and 230 nM for JNK1, JNK2, and JNK3, respectively.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.23%
CAS. Nr.: 848344-36-5
Formel: C₂₅H₂₃N₅O₂S
Molecular Weight:457.55

Speicherung:

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

Bentamapimod Chemical Structure

CAS. Nr.: 848344-36-5

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Bentamapimod (AS 602801) is an ATP-competitive JNK inhibitor with IC₅₀ of 80 nM, 90 nM, and 230 nM for JNK1, JNK2, and JNK3, respectively.

IC₅₀ & Target^[1]

JNK1

80 nM (IC₅₀)

JNK2

90 nM (IC₅₀)

JNK3

230 nM (IC₅₀)

Alle JNK Isoform-spezifische Produkte anzeigen :

In Vitro

Bentamapimod (AS 602801) treatment induces cell death and accordingly decreased the number of viable cells in all three cell lines in a dose-dependent manner, suggesting that Bentamapimod (AS 602801) may have selective cytotoxic activity against neoplastic cells. Bentamapimod (AS 602801) exhibits cytotoxicity against both serum-cultured non-stem cancer cells and cancer stem cells derived from human pancreatic cancer, non-small cell lung cancer, ovarian cancer and glioblastoma at concentrations that did not decrease the viability of normal human fibroblasts. Bentamapimod (AS 602801) also inhibits the self-renewal and tumor-initiating capacity of cancer stem cells surviving Bentamapimod (AS 602801) treatment^[2].

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

In Vivo

Treatment of nude mice bearing xenografts biopsied from women with endometriosis (BWE) with 30 mg/kg Bentamapimod (AS 602801) causes 29% regression of lesion. Medroxyprogesterone acetate (MPA) or progesterone (PR) alone did not cause regression of BWE lesions, but combining 10 mg/kg Bentamapimod (AS 602801) with MPA caused 38% lesion regression. In human endometrial organ cultures (from healthy women), treatment with Bentamapimod (AS 602801) or MPA reduced matrix metalloproteinase-3 (MMP-3) release into culture medium. In organ cultures established with BWE, PR or MPA failed to inhibit MMP-3 secretion, whereas AS 602801 alone or MPA + Bentamapimod (AS 602801) suppresses MMP-3 production. In an autologous rat endometriosis model, AS 602801 causes 48% regression of lesions compared to GnRH antagonist Antide (84%). Bentamapimod (AS 602801) reduces inflammatory cytokines in endometriotic lesions, while levels of cytokines in ipsilateral horns are unaffected. Furthermore, Bentamapimod (AS 602801) enhances natural killer cell activity, without apparent negative effects on uterus^[3].

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

Chemical Information

CAS. Nr. 848344-36-5
Appearance Solid
Molecular Weight 457.55
Formel C₂₅H₂₃N₅O₂S
Color Light yellow to yellow
SMILES

N#CC(C1=NC(OCC2=CC=C(C=C2)CN3CCOCC3)=NC=C1)C4=NC5=CC=CC=C5S4
Synonyms

AS 602801
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (12)

All WB

Sort by:

Journal Impact Factor

Nat Nanotechnol

Therapeutically reprogrammed nutrient signalling enhances nanoparticulate albumin bound drug uptake and efficacy in KRAS-mutant cancer. [Abstract]

2021 Jul;16(7):830-839. PMID: 33958764
Nat Biomed Eng

TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]

2018 Aug;2(8):578-588. PMID: 31015631
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Life Sci

Dapagliflozin promotes metabolic reprogramming against myocardial infarction through the MAPK-FOXO3-STC1 and HIF-1a-STC1 pathways. [Abstract]

2025 Sep 15:377:123798. PMID: 40480620
ACS Omega

The Role and Efficacy of JNK Inhibition in Inducing Lung Cancer Cell Death Depend on the Concentration of Cisplatin. [Abstract]

2024 Jun 18;9(26):28311-28322. PMID: 38973918
J Photochem Photobiol B

Hydroxysafflower yellow a protects against UVA- and UVB-induced skin aging by suppressing cell apoptosis and SASP via targeting JNK and p38 MAPK pathway. [Abstract]

2026 Jan:274:113340. PMID: 41421060
Npj Viruses

JNK kinase regulates phosphorylation of HCoV-229E nucleocapsid protein. [Abstract]

2025 Sep 18;3(1):69. PMID: 40968155
Anticancer Res

AS602801 Sensitizes Ovarian Cancer Stem Cells to Paclitaxel by Down-regulating MDR1. [Abstract]

2019 Feb;39(2):609-617. PMID: 30711936

Bentamapimod purchased from MedChemExpress. Usage Cited in: Anticancer Res. 2019 Feb;39(2):609-617. [Abstract]

A2780 CSLCs are treated with paclitaxel (2 nM) or carboplatin (5 μM) in the presence or absence of AS602801 (7.5 μM) and/or YM155 (10 nM) for 3 days, and then subjected to western blot analysis of survivin and glyceraldehyde 3-phosphate dehydrogenase (GAPDH).

Bentamapimod purchased from MedChemExpress. Usage Cited in: Anticancer Res. 2019 Feb;39(2):609-617. [Abstract]

A2780 CSLCs and TOV-21G CLSCs are treated with AS602801 at 7.5 μM for the indicated time and the cells are subjected to western blot analysis of multidrug resistance protein 1 (MDR1) and glyceraldehyde 3-phosphate dehydrogenase (GAPDH).
Anticancer Res

AS602801, an Anticancer Stem Cell Candidate Drug, Reduces Survivin Expression and Sensitizes A2780 Ovarian Cancer Stem Cells to Carboplatin and Paclitaxel. [Abstract]

2018 Dec;38(12):6699-6706. PMID: 30504379

Bentamapimod purchased from MedChemExpress. Usage Cited in: Anticancer Res. 2018 Dec;38(12):6699-6706. [Abstract]

The protein expression of analysis Survivin with or without the treatment of AS602801 in different times and concentrations.
bioRxiv

2023 Jun 25.
Methods Mol Biol

Methods for High-throughput Drug Combination Screening and Synergy Scoring. [Abstract]

2018:1711:351-398. PMID: 29344898
Oncotarget

The novel JNK inhibitor AS602801 inhibits cancer stem cells in vitro and in vivo. [Abstract]

2016 May 10;7(19):27021-32. PMID: 27027242

Bentamapimod purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 May 10;7(19):27021-32. [Abstract]

AS602801 treatment causes loss of stem cell marker expression in cancer stem cells. Subsequent analysis revealed that the levels of other stem cell markers, such as Sox2, Nanog, and Bmi1, are decreased similarly to CD133.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 8.33 mg/mL (18.21 mM; ultrasonic and warming and heat to 60°C; 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

2.1856 mL

10.9278 mL

21.8555 mL

5 mM

0.4371 mL

2.1856 mL

4.3711 mL

10 mM

0.2186 mL

1.0928 mL

2.1856 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.

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:

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: ≥ 0.83 mg/mL (1.81 mM); Suspended solution

This protocol yields a suspended solution of ≥ 0.83 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.

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

Protokoll

Cell Assay^[2]

PANC-1, A2780, and A549 human cancer cells and IMR90 human normal fibroblasts are treated without (control) or with the indicated concentrations of Bentamapimod (AS 602801) (2.5, 5, and 7.5 μM) for 3 days. The number of viable cells (left panels) and the percentage of dead cells (right panels) are determined using trypan blue as a vital dye^[2].

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

Animal Administration^[3]

Mice^[3]
The 5-week-old athymic (ncr/nude) ovariectomized mice are anesthetized with isoflurane and subcutaneously implanted with a silastic capsule containing 8 μg estradiol. Twenty-four hours later, mice received subcutaneous or intraperitoneal injection with a phosphate-buffered saline (PBS) suspension of 8 to 10 human endometrial tissue fragments/mouse (biopsies obtained from volunteers or patients) on the ventral midline just below the umbilicus. For 24 hours immediately preceding injection, tissue fragments are established as organ cultures treated with 1 nM estradiol, PR, or MPA. Oral administration of Bentamapimod (AS 602801) is initiated 10 to 12 days following the injection of tissue. Progesterone is provided via a slow-release silastic capsule containing 25 μg PR, and MPA is given by twice-weekly injections (200 mg/kg) along the right flank using a tuberculin syringe. Bentamapimod (AS 602801) is administered by gavage at a dose of 10 mg/kg and 30 mg/kg/animal for 30 days. Following the completion of treatment, mice are again anesthetized and sacrificed by cervical dislocation for direct examination of lesion size and number. Uteri are measured and weighed, and excised lesions rapidly frozen for further analysis^[3].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 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]. Messoussi A, et al. Recent progress in the design, study, and development of c-Jun N-terminal kinase inhibitors as anticanceragents. Chem Biol. 2014 Nov 20;21(11):1433-43. [Content Brief]

[2]. Okada M, et al. The novel JNK inhibitor AS602801 inhibits cancer stem cells in vitro and in vivo. Oncotarget. 2016 May 10;7(19):27021-32. [Content Brief]

[3]. Palmer SS, et al. Bentamapimod (JNK Inhibitor AS602801) Induces Regression of Endometriotic Lesions in Animal Models. Reprod Sci. 2016 Jan;23(1):11-23. [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	2.1856 mL	10.9278 mL	21.8555 mL	54.6388 mL
	5 mM	0.4371 mL	2.1856 mL	4.3711 mL	10.9278 mL
	10 mM	0.2186 mL	1.0928 mL	2.1856 mL	5.4639 mL
	15 mM	0.1457 mL	0.7285 mL	1.4570 mL	3.6426 mL

Keywords

Bentamapimod

12 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Bentamapimod

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Parkinson's Disease Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Rare Diseases Drug Library

Antidepressant Compound Library

Anti-Pulmonary Fibrosis Compound Library

Pain-Related Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Bentamapimod

Alle JNK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bentamapimod Related Classifications

HY-14761 Related Classifications