BMX-IN-1
Based on 7 publication(s) in Google Scholar
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.
- Purity: 98.90%
- CAS No.: 1431525-23-3
- Formula: C29H24N4O4S
- Molecular Weight:524.59
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) BMX-IN-1
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Cancer Lett. 2021 Dec 1:522:93-104. [Abstract]
- Int J Biol Macromol. 2026 Feb;344(Pt 1):150362. [Abstract]
- JCI Insight. 2024 Jul 22;9(14):e169647. [Abstract]
- Cell Mol Bioeng. 2022 Apr 18;15(3):231-243. [Abstract]
- Oncotarget. 2017 Jul 25;8(30):49238-49252. [Abstract]
- Harvard Medical School LINCS LIBRARY
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WB
Biological Activity
IC50: 8 nM (BMX), 10.4 nM (BTK)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | GI50 |
>10 μM
Compound: Chemical Probe: BMX-IN-1, QL-XII-61
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Cytotoxicity against mouse BaF3 cells assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
Cytotoxicity against mouse BaF3 cells assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
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[PMID: 23594111] |
| BaF3 | GI50 |
0.025 μM
Compound: Chemical Probe: BMX-IN-1, QL-XII-61
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Antiproliferative activity against mouse BaF3 cells expressing TEL-fused BMX assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing TEL-fused BMX assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
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[PMID: 23594111] |
| BaF3 | GI50 |
3.64 μM
Compound: Chemical Probe: BMX-IN-1, QL-XII-61
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Antiproliferative activity against mouse BaF3 cells expressing TEL-fused BLK assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing TEL-fused BLK assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
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[PMID: 23594111] |
| BaF3 | GI50 |
4.92 μM
Compound: Chemical Probe: BMX-IN-1, QL-XII-61
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Antiproliferative activity against mouse BaF3 cells expressing TEL-fused JAK1 assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing TEL-fused JAK1 assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
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[PMID: 23594111] |
| BaF3 | GI50 |
5.83 μM
Compound: Chemical Probe: BMX-IN-1, QL-XII-61
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Antiproliferative activity against mouse BaF3 cells expressing TEL-fused JAK2 assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing TEL-fused JAK2 assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
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[PMID: 23594111] |
| BaF3 | GI50 |
6.09 μM
Compound: Chemical Probe: BMX-IN-1, QL-XII-61
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Antiproliferative activity against mouse BaF3 cells expressing TEL-fused TYK2 E9757D mutant assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing TEL-fused TYK2 E9757D mutant assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
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[PMID: 23594111] |
| BaF3 | GI50 |
7.98 μM
Compound: Chemical Probe: BMX-IN-1, QL-XII-61
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Antiproliferative activity against mouse BaF3 cells expressing TEL-fused JAK3 assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing TEL-fused JAK3 assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
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[PMID: 23594111] |
| BaF3 | IC50 |
>10 μM
Compound: Chemical Probe: BMX-IN-1, QL-XII-61
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Antiproliferative activity against mouse BaF3 cells expressing TEL-fused BMX Cys496Ser assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing TEL-fused BMX Cys496Ser assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
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[PMID: 23594111] |
| BaF3 | IC50 |
25 nM
Compound: BMX-IN-1
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Antiproliferative activity against TEL-BMX transformed mouse BaF3 cells assessed as inhibition of cell proliferation
Antiproliferative activity against TEL-BMX transformed mouse BaF3 cells assessed as inhibition of cell proliferation
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[PMID: 37437350] |
| BaF3 | IC50 |
569 nM
Compound: Chemical Probe: BMX-IN-1, QL-XII-61
|
Antiproliferative activity against mouse BaF3 cells expressing TEL-fused BMX assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells expressing TEL-fused BMX assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
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[PMID: 23594111] |
| DU-145 | GI50 |
4.38 μM
Compound: Chemical Probe: BMX-IN-1, QL-XII-61
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Antiproliferative activity against human DU-145 cells assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
Antiproliferative activity against human DU-145 cells assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
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[PMID: 23594111] |
| LNCaP C4-2 | GI50 |
>10 μM
Compound: Chemical Probe: BMX-IN-1, QL-XII-61
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Antiproliferative activity against human C4-2 cells assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
Antiproliferative activity against human C4-2 cells assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
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[PMID: 23594111] |
| PC-3 | GI50 |
5.37 μM
Compound: Chemical Probe: BMX-IN-1, QL-XII-61
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Antiproliferative activity against human PC-3 cells assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
Antiproliferative activity against human PC-3 cells assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
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[PMID: 23594111] |
| VCaP | GI50 |
2.46 μM
Compound: Chemical Probe: BMX-IN-1, QL-XII-61
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Antiproliferative activity against human VCaP cells assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
Antiproliferative activity against human VCaP cells assessed growth inhibition incubated for 2 to 5 days by CellTiter-Glo assay
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[PMID: 23594111] |
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.
Chemical Information
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CAS No. 1431525-23-3
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Appearance Solid
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Molecular Weight 524.59
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Formula C29H24N4O4S
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Color White to yellow
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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
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Synonyms
BMX kinase inhibitor
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Cancer Lett
Fas signaling in adipocytes promotes low-grade inflammation and lung metastasis of colorectal cancer through interaction with Bmx. [Abstract]2021 Dec 1:522:93-104. PMID: 34536556 -
Int J Biol Macromol
Bone marrow tyrosine kinase on chromosome X promotes epithelial-mesenchymal transition through signal transducer and activator of transcription 3 in colorectal cancer. [Abstract]2026 Feb;344(Pt 1):150362. PMID: 41565140 -
JCI Insight
Preclinical spheroid models identify BMX as a therapeutic target for metastatic MYCN nonamplified neuroblastoma. [Abstract]2024 Jul 22;9(14):e169647. PMID: 39133652 -
Cell Mol Bioeng
Ibrutinib Inhibits BMX-Dependent Endothelial VCAM-1 Expression In Vitro and Pro-Atherosclerotic Endothelial Activation and Platelet Adhesion In Vivo. [Abstract]2022 Apr 18;15(3):231-243. PMID: 35611166 -
Oncotarget
BMX/Etk promotes cell proliferation and tumorigenicity of cervical cancer cells through PI3K/AKT/mTOR and STAT3 pathways. [Abstract]2017 Jul 25;8(30):49238-49252. PMID: 28514765
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.
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Harvard Medical School LINCS LIBRARY
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (19.06 mM); Suspended solution; Need ultrasonic
Protocol
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
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 |