BMX-IN-1
BMX-IN-1 is a highly selective and irreversible inhibitor of BMX kinase [1].
BMX, also known as ETK, is a member of Tec family and plays an important role in regulating ischemia-mediated arteriogenesis and lymphangiogenesis. BMX is mainly expressed in arterial endothelia and in myeloid hematopoietic cells and it has been reported that BMX involves in tumor growth [2].
BMX-IN-1 is a potent BMX kinase inhibitor and has an irreversible function on BMX kinase. When tested with prostate cancer cell lines, BMX-IN-1 treatment inhibited the proliferation of Tel-BMX-transformed Ba/F3 cells at lowdose [1].
References:
[1].Liu, F., et al., Discovery of a selective irreversible BMX inhibitor for prostate cancer. ACS Chem Biol, 2013. 8(7): p. 1423-8.
[2].Holopainen, T., et al., Deletion of the endothelial Bmx tyrosine kinase decreases tumor angiogenesis and growth. Cancer Res, 2012. 72(14): p. 3512-21.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 524.59 |
| Cas No. | 1431525-23-3 |
| Formula | C29H24N4O4S |
| Synonyms | BMX kinase inhibitor |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥5.25 mg/mL in DMSO |
| Chemical Name | N-[5-[9-[4-(methanesulfonamido)phenyl]-2-oxobenzo[h][1,6]naphthyridin-1-yl]-2-methylphenyl]prop-2-enamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(C=C(C=C1)N2C(=O)C=CC3=CN=C4C=CC(=CC4=C32)C5=CC=C(C=C5)NS(=O)(=O)C)NC(=O)C=C |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Kinase experiment [1]: | |
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Kinase assay |
The serially diluted BMX-IN-1 was added to the BTK kinase. After 30 min incubation at RT, ATP (final concentration: 20μM) was added and incubated for 20 min at 37°C. The reactions were stopped by addition of 5X sample buffer. Then the phosphorylation of BTK was detected by western-blot using a pBTK Y551 antibody (BD). |
| Cell experiment [1]: | |
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Cell lines |
Ramos cell line |
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Preparation method |
The solubility of this compound in DMSO is >5.3 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.3, 1, 3 and 10 uM for 16/24/48 hours. |
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Applications |
In Ramos cell line, BMX-IN-1 significantly inhibited cell cycle progression at G0/G1 in a dose-dependent manner at 24h and strongly induced apoptosis at a concentration of 1 μM at 8h, while with a longer drug exposure (24 hours), a concentration of 300 nM was sufficient to induce apoptosis. |
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References: [1]. Hong Wu, et al. Discovery of a Potent, Covalent BTK Inhibitor for B-Cell Lymphoma. ACS Chem Biol. 2014 May 16; 9(5): 1086–1091. | |
| Description | BMX-IN-1 is a highly selective and potent irreversible inhibitor of BMX kinase. | |||||
| Targets | BMX Kinase | |||||
| IC50 | ||||||
Quality Control & MSDS
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Chemical structure
