1. Protein Tyrosine Kinase/RTK
  2. Btk
    BMX Kinase

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

Cat. No.: HY-80002 Purity: 98.88%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 235 In-stock
Estimated Time of Arrival: December 31
2 mg USD 114 In-stock
Estimated Time of Arrival: December 31
5 mg USD 204 In-stock
Estimated Time of Arrival: December 31
10 mg USD 360 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1188 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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

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

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

    HeLa and SiHa cells are treated with DMSO and LFM-A13, a pharmacologic inhibitor of BMX, and the phosphorylation and total BMX levels are determined using a western blot analysis.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    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].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 20 mg/mL (38.13 mM)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.1906 mL 0.9531 mL 1.9063 mL
    *Please refer to the solubility information to select the appropriate solvent.
    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
    Molecular Weight

    524.59

    Formula

    C₂₉H₂₄N₄O₄S

    CAS No.

    1431525-23-3

    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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 98.88%

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    Product Name:
    BMX-IN-1
    Cat. No.:
    HY-80002
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    BMX-IN-1

    Cat. No.: HY-80002