2. MAPK/ERK Pathway
  3. JNK
  4. Bentamapimod

Bentamapimod  (Synonyms: AS 602801)

Cat. No.: HY-14761 Purity: 99.32%
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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.

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

Bentamapimod Chemical Structure

Bentamapimod Chemical Structure

CAS No. : 848344-36-5

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 85 In-stock
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10 mM * 1 mL in DMSO USD 85 In-stock
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5 mg USD 77 In-stock
10 mg USD 132 In-stock
50 mg USD 275 In-stock
100 mg USD 495 In-stock
500 mg USD 1650 In-stock
1 g USD 2970 In-stock
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Customer Review

Based on 12 publication(s) in Google Scholar

Bentamapimod Related Antibodies

Top Publications Citing Use of Products

    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).

    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. 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.

    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.

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    JNK1 JNK2 JNK3 JNK

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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)

    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.

    Bentamapimod Related Antibodies
    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.
    Molecular Weight

    457.55

    Formula

    C25H23N5O2S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1856 mL 10.9278 mL 21.8555 mL
    5 mM 0.4371 mL 2.1856 mL 4.3711 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, 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

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

    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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.32%

    COA (247 KB) LCMS (276 KB)

    Handling Instructions (2659 KB)
    References
    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].

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 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
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    Bentamapimod 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:

    Bentamapimod848344-36-5AS 602801AS602801AS-602801JNKc-Jun N-terminal kinaseInhibitorinhibitorinhibit

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