BMH-21

Catalog No.S7718 Batch:S771803

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Technical Data

Formula

C21H20N4O2
Molecular Weight 360.41 CAS No. 896705-16-1
Solubility (25°C)* In vitro DMSO 6 mg/mL (16.64 mM)
Ethanol 2 mg/mL (5.54 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description BMH-21 is a DNA intercalator, which binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription.
Targets
RNA polymerase I [1]
In vitro

BMH-21 causes proteasome-dependent destruction of RPA194, the large catalytic subunit protein of Pol I holocomplex. [1]

In U2OS cancer cell line, BMH-21 results in degradation of RPA194 and translocation of NCL with IC50 of 0.05 μM and 0.07 μM, respectively. By causing nucleolar stress, BMH-21 also shows potent inhibition on cell viability. [2]
In vivo

BMH-21 reduces tumor growth in mouse xenografts. [1]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    U2OS osteosarcoma cells

  • Concentrations

    ~5 μM

  • Incubation Time

    48 hours

  • Method

    The cells are maintained at 37 °C in a humidified atmosphere containing 5% CO2. U2OS osteosarcoma cells are cultured in DMEM supplemented with 15% fetal bovine serum. Cells are plated in 96-well plates at a density of 10000 cells/well in triplicate and incubated for 48 h with the compounds. Viability is determined using WST-1 cell proliferation reagent.
Animal Study:

[3]
  • Animal Models

    Athymic NCr nu/nu mice

  • Dosages

    25 or 50 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Cell, 2018, 174(2):338-349]

Selleck's BMH-21 has been cited by 21 publications

DNA-PK participates in pre-rRNA biogenesis independent of DNA double-strand break repair [ Nucleic Acids Res, 2024, gkae316] PubMed: 38682589
Monoallelically expressed noncoding RNAs form nucleolar territories on NOR-containing chromosomes and regulate rRNA expression [ Elife, 2024, 13e80684] PubMed: 38240312
Pre-rRNA facilitates the recruitment of RAD51AP1 to DNA double-strand breaks [ J Biol Chem, 2024, 300(3):107115] PubMed: 38403248
CX‑5461 potentiates imatinib‑induced apoptosis in K562 cells by stimulating KIF1B expression [ Exp Ther Med, 2024, 27(3):107.] PubMed: 38356673
CX‑5461 potentiates imatinib‑induced apoptosis in K562 cells by stimulating KIF1B expression [ Exp Ther Med, 2024, 27(3):107] PubMed: 38356673
The ribosomal protein L22 binds the MDM4 pre-mRNA and promotes exon skipping to activate p53 upon nucleolar stress [ bioRxiv, 2024, 10.1101/2023.12.29.573614] PubMed: none
The ribosomal protein L22 binds the MDM4 pre-mRNA and promotes exon skipping to activate p53 upon nucleolar stress [ bioRxiv, 2024, 10.1101/2023.12.29.573614] PubMed: none
The BRCA1/BARD1 complex recognizes pre-ribosomal RNA to facilitate homologous recombination [ Cell Discov, 2023, 9(1):99] PubMed: 37789001
The BRCA1/BARD1 complex recognizes pre-ribosomal RNA to facilitate homologous recombination [ Cell Discov, 2023, 9(1):99] PubMed: 37789001
Ribosome biosynthesis and Hedgehog activity are cooperative actionable signaling mechanisms in breast cancer following radiotherapy [ NPJ Precis Oncol, 2023, 7(1):61] PubMed: 37380890

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.