1. Protein Tyrosine Kinase/RTK
  2. Btk BMX Kinase
  3. BMX-IN-1

BMX-IN-1  (Synonyms: BMX kinase inhibitor)

Cat. No.: HY-80002 Purity: 99.84%
COA Handling Instructions

BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.

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

BMX-IN-1 Chemical Structure

BMX-IN-1 Chemical Structure

CAS No. : 1431525-23-3

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 196 In-stock
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10 mg USD 252 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    BMX-IN-1 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 25;8(30):49238-49252.  [Abstract]

    Western blot results show that the expression of BMX is decreased in both BMX-IN-1-treated HeLa and SiHa cells.
    • Biological Activity

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    • Purity & Documentation

    • References

    • Customer Review

    Description

    BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.

    IC50 & Target

    IC50: 8 nM (BMX), 10.4 nM (BTK)

    In Vitro

    BMX-IN-1 inhibits the proliferation of Tel-BMX-transformed Ba/F3 cells and RV-1 cells with IC50s of 25 nM and 2.53 μM. BMX-IN-1 exhibits remarkable selectivity with an S(10) score of 0.01. BMX-IN-1 inhibits only wild-type BMX with an IC50 of 138 nM. BMX-IN-1 requires covalent modification of Cys496 of BMX to achieve potent inhibition[1].

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

    Molecular Weight

    524.59

    Formula

    C29H24N4O4S

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C1N(C2=C(C=C1)C=NC3=CC=C(C4=CC=C(NS(=O)(C)=O)C=C4)C=C32)C5=CC=C(C)C(NC(C=C)=O)=C5

    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: 

    DMF : 10 mg/mL (19.06 mM; Need ultrasonic)

    DMSO : 8.33 mg/mL (15.88 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 1.9063 mL 9.5313 mL 19.0625 mL
    5 mM 0.3813 mL 1.9063 mL 3.8125 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

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    (per animal)

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.84%

    References
    Cell Assay
    [1]

    RV-1 cells in complete or serum-reduced DMEM are treated with DMSO, BMX-IN-1 (2.5 μM), MK2206 (200 nM), or the combination of BMX-IN-1 and MK2206 for 5 days before cells are harvested by trypsin and washed with cold PBS. The cells are then fixed in 70% cold ethanol (prechilled at −20°C) and incubated at 4°C overnight. On the day of flow cytometry, cells are collected by centrifugation, washed with PBS, and stained in 50 μg/mL propidium iodide + 0.5 mg/mL RNase in PBS + 0.5% Triton-X100 for 30 min at RT and moved to 4°C until the time of analysis. Flow cytometry is performed using a BD FACScan, and results are analyzed by ModFit software in the Flow Cytometry Core Facility in Dana-Faber Cancer Institute.

    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 / DMF 1 mM 1.9063 mL 9.5313 mL 19.0625 mL 47.6563 mL
    5 mM 0.3813 mL 1.9063 mL 3.8125 mL 9.5313 mL
    10 mM 0.1906 mL 0.9531 mL 1.9063 mL 4.7656 mL
    15 mM 0.1271 mL 0.6354 mL 1.2708 mL 3.1771 mL
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    BMX-IN-1 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.

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    Product Name:
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    Cat. No.:
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