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Description: Potent and irreversible BMX inhibitor
Chemical Name: N-[2-Methyl-5-[9-[4-[(methylsulfonyl)amino]phenyl]-2-oxobenzo[h]-1,6-naphthyridin-1(2H)-yl]phenyl]-2-propenamide
Purity: ≥98% (HPLC)
Citations (1)

Biological Activity for BMX-IN-1

BMX-IN-1 is a potent and irreversible BMX inhibitor (IC50 = 25 nM). Covalently modifies Cysteine 496. Demonstrates selectivity over other Tec family members with identically positioned reactive cysteine residue in vitro. Reduces cell number and induces apoptosis in prostate cancer cell lines. Also inhibits proliferation and reduces viability in HeLa and SiHa cell lines.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

External Portal Information for BMX-IN-1 is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of BMX-IN-1 is reviewed on the chemical probes website.

Technical Data for BMX-IN-1

M. Wt 524.59
Formula C29H24N4O4S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1431525-23-3
PubChem ID 71576693
Smiles CC(C=C5)=C(NC(C=C)=O)C=C5N(C2=C(C=C3)C=NC1=CC=C(C4=CC=C(NS(=O)(C)=O)C=C4)C=C12)C3=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for BMX-IN-1

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 0.52 1 with gentle warming

Preparing Stock Solutions for BMX-IN-1

The following data is based on the product molecular weight 524.59. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.01 mM 190.63 mL 953.13 mL 1906.25 mL
0.05 mM 38.13 mL 190.63 mL 381.25 mL
0.1 mM 19.06 mL 95.31 mL 190.63 mL
0.5 mM 3.81 mL 19.06 mL 38.13 mL

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References for BMX-IN-1

References are publications that support the biological activity of the product.

Liu et al (2013) Discovery of a selective irreversible BMX inhibitor for prostate cancer. ACS Chem.Biol. 8 1423 PMID: 23594111

Li et al (2017) BMX/Etk promotes cell proliferation and tumorigenicity of cervical cancer cells through PI3K/AKT/mTOR and STAT3 pathways. Oncotarget. 8 49238 PMID: 28514765

If you know of a relevant reference for BMX-IN-1, please let us know.

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Keywords: BMX-IN-1, BMX-IN-1 supplier, BMX, inhibitors, inhibits, nonreceptor, tyrosine, kinase, potent, irreversible, selective, Other, Kinases, 5123, Tocris Bioscience

1 Citation for BMX-IN-1

Citations are publications that use Tocris products. Selected citations for BMX-IN-1 include:

Rudolf et al (2021) Probing the signaling requirements for naive human pluripotency by high-throughput chemical screening. Cell Rep 35 109233 PMID: 34133938

Do you know of a great paper that uses BMX-IN-1 from Tocris? Please let us know.

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