BMH-21

BMH-21 is a DNA intercalator, which binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription.

BMH-21 Chemical Structure

BMH-21 Chemical Structure

CAS No. 896705-16-1

Purity & Quality Control

BMH-21 Related Products

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
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]

Cell Research 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.

Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability 28656213
Western blot Bax / Caspase-3 / Cleaved caspase-3 MDM2 / p53 / p-p53 28656213
Immunofluorescence Fibrillarin Nuclephosmin 28656213
In Vivo
In vivo

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

Animal Research Animal Models Athymic NCr nu/nu mice
Dosages 25 or 50 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 360.41 Formula

C21H20N4O2

CAS No. 896705-16-1 SDF Download BMH-21 SDF
Smiles CN(C)CCNC(=O)C1=CC=CN2C1=NC3=CC4=CC=CC=C4C=C3C2=O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 6 mg/mL ( (16.64 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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