1431525-23-3
1431525-23-3 structure
- Name: BMX-IN-1
- Chemical Name: BMX-IN-1
- CAS Number: 1431525-23-3
- Molecular Formula: C29H24N4O4S
- Molecular Weight: 524.590
- Catalog: Biochemical Inhibitor Protein tyrosine kinase
- Create Date: 2018-06-20 17:30:00
- Modify Date: 2024-01-02 16:35:59
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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.
| Name | BMX-IN-1 |
|---|---|
| Synonyms |
2-Propenamide, N-[2-methyl-5-[9-[4-[(methylsulfonyl)amino]phenyl]-2-oxobenzo[h][1,6]naphthyridin-1(2H)-yl]phenyl]-
MFCD25372042 BMX-IN-1 N-{2-Methyl-5-[9-{4-[(methylsulfonyl)amino]phenyl}-2-oxobenzo[h][1,6]naphthyridin-1(2H)-yl]phenyl}acrylamide |
| 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. |
|---|---|
| Related Catalog | |
| 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]. |
| Cell Assay | 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. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Molecular Formula | C29H24N4O4S |
| Molecular Weight | 524.590 |
| Exact Mass | 524.151855 |
| LogP | 3.52 |
| Index of Refraction | 1.708 |
| Storage condition | 2-8℃ |