1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. BCI-215

BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells.

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

CAS No. : 1245792-67-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
Cell Proliferation/Viability Assay
RT-PCR
WB
Cell Imaging/Staining

    BCI-215 purchased from MedChemExpress. Usage Cited in: Molecules. 2022 Aug 25;27(17):5449.  [Abstract]

    The cytotoxicity of the BCI-215 exposure in the B16F10 cells was assessed using a WST cell proliferation assay and 10 µM BCI-215 showed cytotoxic effects.

    BCI-215 purchased from MedChemExpress. Usage Cited in: Molecules. 2022 Aug 25;27(17):5449.  [Abstract]

    Relative value of MITF mRNA. BCI-215 (1 μM) decreased the transcription of MITF modestly only at an early time point.

    BCI-215 purchased from MedChemExpress. Usage Cited in: Molecules. 2022 Aug 25;27(17):5449.  [Abstract]

    Immunoblotting of MITF and Tyrosinase up to 6 h after a treatment with BCI-215 (1 μM).

    BCI-215 purchased from MedChemExpress. Usage Cited in: Molecules. 2022 Aug 25;27(17):5449.  [Abstract]

    Fontana–Masson staining of ex vivo human cultured skin tissue treated with a 200 mJ/cm2 dose of UVB with or without the BCI-215 (100 nM) treatment.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells[1][2].

    IC50 & Target

    DUSP-MKP[1]

    In Vitro

    BCI-215 concentration-dependently increases pERK levels in DUSP-overexpressing cells with IC50 value in the micromolar range[1].
    BCI-215 (1-20 μM; 6 hours) retains fibroblast growth factor hyperactivating and cellular DUSP6/MKP-3 and DUSP1/MKP-1 inhibitory activity but is nontoxic to zebrafish embryos and an endothelial cell line[1].
    BCI-215 inhibits survival and motility of MDA-MB-231 human breast cancer cells but does not affect viability of cultured hepatocytes[2].
    BCI-215 is completely devoid of hepatocyte toxicity up to 100 μM[2].
    BCI-215 does not generate ROS in hepatocytes or in developing Zebrafish larvae. BCI-215 (22 μM) has antimigratory and proapoptotic activities in breast cancer cells that correlate with induction of ERK phosphorylation[2].
    BCI-215 (20 μM; 1 hour) induces mitogenic and stress signaling in cancer cells without generating ROS[2].

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

    Apoptosis Analysis [2]

    Cell Line: MDA-MB-231 cells
    Concentration: 22 µM
    Incubation Time:
    Result: Caused apoptotic cell death at concentrations that induce ERK phosphorylation.

    Western Blot Analysis[2]

    Cell Line: MDA-MB-231 cells
    Concentration: 20 µM
    Incubation Time: 1 hour
    Result: Induced a stress response that is not dependent on oxidation.
    Molecular Weight

    396.32

    Formula

    C22H22BrNO

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C1/C(C(NC2CCCCC2)C3=C1C=CC(Br)=C3)=C/C4=CC=CC=C4

    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 : 33.33 mg/mL (84.10 mM; Need ultrasonic; 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 2.5232 mL 12.6161 mL 25.2321 mL
    5 mM 0.5046 mL 2.5232 mL 5.0464 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
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    Concentration
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    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

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    Volume (start)

    V1

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    C2

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    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 (2.09 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

      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.
    • Protocol 2

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

      Solubility: ≥ 0.83 mg/mL (2.09 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.83 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 (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

    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: 99.86%

    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 2.5232 mL 12.6161 mL 25.2321 mL 63.0803 mL
    5 mM 0.5046 mL 2.5232 mL 5.0464 mL 12.6161 mL
    10 mM 0.2523 mL 1.2616 mL 2.5232 mL 6.3080 mL
    15 mM 0.1682 mL 0.8411 mL 1.6821 mL 4.2054 mL
    20 mM 0.1262 mL 0.6308 mL 1.2616 mL 3.1540 mL
    25 mM 0.1009 mL 0.5046 mL 1.0093 mL 2.5232 mL
    30 mM 0.0841 mL 0.4205 mL 0.8411 mL 2.1027 mL
    40 mM 0.0631 mL 0.3154 mL 0.6308 mL 1.5770 mL
    50 mM 0.0505 mL 0.2523 mL 0.5046 mL 1.2616 mL
    60 mM 0.0421 mL 0.2103 mL 0.4205 mL 1.0513 mL
    80 mM 0.0315 mL 0.1577 mL 0.3154 mL 0.7885 mL
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    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.

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    Product Name:
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    Cat. No.:
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