BMH-21 DNA/RNA Synthesis inhibitor

Cat.No.S7718

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

Chemical Structure

Molecular Weight: 360.41

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 360.41 Formula

C21H20N4O2

Storage (From the date of receipt)
CAS No. 896705-16-1 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN(C)CCNC(=O)C1=CC=CN2C1=NC3=CC4=CC=CC=C4C=C3C2=O

Solubility

In vitro
Batch:

DMSO : 2 mg/mL (5.54 mM) Warmed with 50°C water bath; Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
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, this compound results in degradation of RPA194 and translocation of NCL with IC50 of 0.05 μM and 0.07 μM, respectively. By causing nucleolar stress, it also shows potent inhibition on cell viability. [2]

In vivo

This compound reduces tumor growth in mouse xenografts. [1]

References

Applications

Methods Biomarkers Images PMID
Growth inhibition assay Cell viability S7718-viability1 28656213
Western blot Bax / Caspase-3 / Cleaved caspase-3 MDM2 / p53 / p-p53 S7718-WB1 28656213
Immunofluorescence Fibrillarin Nuclephosmin S7718-IF1 28656213

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