2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. 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.

CAS No. : 896705-16-1

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Customer Review

Based on 14 publication(s) in Google Scholar

BMH-21 Related Antibodies

Top Publications Citing Use of Products

    BMH-21 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2025 Mar 6;85(5):894-912.e10.  [Abstract]

    BMH-21 (10 μM; 6 h) decreased MCL1, CCND3, and MYB similarly regardless of SLFN11 in CCRF-CEM cells.

    BMH-21 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2025 Mar 6;85(5):894-912.e10.  [Abstract]

    BMH-21 (10 μM) activated apoptosis independently of SLFN11 in CCRF-CEM cells, with similar kinetics to SLFN11-dependent apoptosis.

    BMH-21 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2025 Mar 6;85(5):894-912.e10.  [Abstract]

    The RNA polymerase I (POLR1) inhibitors BMH-21 (10 µM; 6 h) drastically reduced EU incorporation in leukemia MOLT4 irrespective of SLFN11 expression.

    BMH-21 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Dec 20;23(1):275.  [Abstract]

    BMH-21 (5 µM) caused a significant delay in growth of mouse fibrosarcoma MCA205 cells and kept a significant percentage of mice alive and tumor-free.

    BMH-21 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Dec 20;23(1):275.  [Abstract]

    Systemic treatment of mice bearing established tumors with BMH-21 (50 mg/kg; i.p.) significantly reduced tumor progression, and this effect was lost upon in vivo depletion of T cells by monoclonal antibodies specific for CD4 and CD8.

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    RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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

    RNA Polymerase

     

    Cellular Effect
    Cell Line Type Value Description References
    HeLa IC50
    0.46 μM
    Compound: BMH-21
    Cytotoxicity against human HeLa cells
    Cytotoxicity against human HeLa cells
    		[PMID: 34124673]
    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.

    BMH-21 Related Antibodies

    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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

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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:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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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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    BMH-21 Related Classifications

    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.

    Keywords:

    BMH-21896705-16-1BMH21BMH 21DNA/RNA SynthesisDNAintercalationdamageresponsetranscriptionRNApolymeraseInucleolusInhibitorinhibitorinhibit

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