1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis
  3. BMH-21

BMH-21 is a first-in-class DNA intercalator which inhibits RNA polymerase I (Pol I) transcription. BMH-21 possesses anticancer activity.

For research use only. We do not sell to patients.

BMH-21 Chemical Structure

BMH-21 Chemical Structure

CAS No. : 896705-16-1

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Customer Review

Based on 7 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

BMH-21 is a first-in-class DNA intercalator which inhibits RNA polymerase I (Pol I) transcription. BMH-21 possesses anticancer activity[1][2].

IC50 & Target
Cellular Effect
Cell Line Type Value Description References
U2OS IC50
0.05 μM
Compound: 2, BMH-21
Induction of RNA polymerase-1 RPA194 subunit degradation in human U2OS cells after 3 hrs by epifluorescence microscopic analysis
Induction of RNA polymerase-1 RPA194 subunit degradation in human U2OS cells after 3 hrs by epifluorescence microscopic analysis
[PMID: 24847734]
U2OS IC50
0.07 μM
Compound: 2, BMH-21
Inhibition of RNA polymerase-1 in human U2OS cells assessed as decrease in nucleolar localization of nucleolin after 3 hrs by epifluorescence microscopic analysis
Inhibition of RNA polymerase-1 in human U2OS cells assessed as decrease in nucleolar localization of nucleolin after 3 hrs by epifluorescence microscopic analysis
[PMID: 24847734]
In Vitro

BMH-21 binds ribosomal DNA and inhibits Pol I transcription[1].
? BMH-21 inhibits RNA polymerase I independent of DNA damage response[1].
? BMH-21 intercalates into double strand (ds) DNA and has binding preference towards GC-rich DNA sequences[1].
? BMH-21 (1 μM; 3 hours) acts in a DNA damage independent manner to activate nucleolar stress and RPA194 degradation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: U2OS cells
Concentration: 0 μM, 0.1 μM , 1 μM, 10 μM
Incubation Time: 48 hours
Result: Decreased the viability of cells at concentrations that activated the DNA damage response.

Western Blot Analysis[1]

Cell Line: A375 cells
Concentration: 1 μM
Incubation Time: 3 hours
Result: Degraded RPA194 with blocked ATM and DNA-PKcs activity.
In Vivo

BMH-21 (50 mg/kg; i.p.; daily; for 6 days) inhibits HCT116 colon cancer tumor growth in vivo[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-week old athymic NCr nu/nu mice, with HCT116 colorectal carcinoma xenograft[2]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection, daily, for 6 days
Result: Significantly inhibited HCT116 colon cancer tumor growth.
Molecular Weight

360.41

Formula

C21H20N4O2

CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

O=C(C1=CC=CN2C1=NC3=C(C=C4C(C=CC=C4)=C3)C2=O)NCCN(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 1 mg/mL (2.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7746 mL 13.8731 mL 27.7462 mL
5 mM --- --- ---
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 25 mg/mL (69.37 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 1 mM 2.7746 mL 13.8731 mL 27.7462 mL 69.3654 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
BMH-21
Cat. No.:
HY-12484
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