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 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
2 mg USD 114 In-stock
5 mg USD 204 In-stock
10 mg USD 360 In-stock
50 mg USD 1188 In-stock
100 mg USD 1680 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • 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 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].

References
Preparing Stock Solutions
Concentration Volume 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.
Cell Assay
[1]

BMX-IN-1 is dissolved in DMSO.

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

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.88%

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