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Chemical Structure| 896705-16-1 Chemical Structure| 896705-16-1

Structure of BMH-21
CAS No.: 896705-16-1

Chemical Structure| 896705-16-1

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BMH-21 is a DNA intercalator that binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription and does not cause phosphorylation of H2AX.

Synonyms: BMH-21

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Product Details of BMH-21

CAS No. :896705-16-1
Formula : C21H20N4O2
M.W : 360.41
SMILES Code : O=C1N2C(C(C(NCCN(C)C)=O)=CC=C2)=NC3=CC4=CC=CC=C4C=C31
Synonyms :
BMH-21
MDL No. :MFCD27225377
InChI Key :BXYDVWIAGDJBEC-UHFFFAOYSA-N
Pubchem ID :3508054

Safety of BMH-21

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of BMH-21

DNA

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
RKO cells 1 μM 3 h Induced degradation of POLR2A Nucleic Acids Res. 2024 May 8;52(8):4151-4166.
Pediatric high-grade glioma cell lines 0.5-2.0 µM 72 h BMH-21 showed significant growth inhibition and apoptosis induction in pediatric glioma cell lines. Neuro Oncol. 2023 Jun 2;25(6):1058-1072
Adult high-grade glioma cell lines 0.15-2.0 µM 72 h BMH-21 significantly reduced glioma cell viability, induced apoptosis, and was effective in both p53-dependent and independent pathways. Neuro Oncol. 2023 Jun 2;25(6):1058-1072
4T1 cells 0.1 µM 48 h To evaluate the synergistic effect of BMH-21 with fisetin, results showed BMH-21 was more effective than fisetin alone, but the combination significantly reduced colony formation ability. Lab Invest. 2021 Nov;101(11):1439-1448
RPMI-7951 melanoma cells 1 μM 4 h FBXL14 overexpression activated BMH-21-mediated RPA194 degradation J Biol Chem. 2022 Dec;298(12):102690
HAP1 chronic myelogenous leukemia cells 1 μM 16 h FBXL14 knockout cells showed significant reduction in BMH-21-induced RPA194 degradation, FBXL14 re-expression restored degradation J Biol Chem. 2022 Dec;298(12):102690
A375 melanoma cells 1 μM 4 h Validated the role of FBXL14 in BMH-21-induced RPA194 degradation, FBXL14 knockdown significantly inhibited degradation J Biol Chem. 2022 Dec;298(12):102690
U2OS osteosarcoma cells 1 μM 4 h Identified FBXL14 as an E3 ligase for RPA194 through RNAi screening, BMH-21 treatment induced RPA194 degradation J Biol Chem. 2022 Dec;298(12):102690
Trypanosoma brucei 427 134 nM 72 h BMH-21 showed selective toxicity against T. brucei proliferation with an IC50 of 134 nM. PLoS Negl Trop Dis. 2017 Mar 6;11(3):e0005432
A375 melanoma cells 1 μM 3 h To evaluate the effect of BMH-21 on rRNA synthesis, results showed that BMH-21 significantly inhibited rRNA synthesis. Cancer Cell. 2014 Jan 13;25(1):77-90
NCI60 cancer cell lines 160 nM 24 h To evaluate the effect of BMH-21 on cancer cell growth and survival, results showed that BMH-21 effectively inhibited cancer cell growth and induced cell death. Cancer Cell. 2014 Jan 13;25(1):77-90
BJ fibroblasts 1 μM 3 h Induced degradation of POLR2A without affecting POLR1A degradation Nucleic Acids Res. 2024 May 8;52(8):4151-4166.
U2OS cells 1 μM 3 h Induced degradation of POLR2A, reduced phosphorylation of Ser5 and Ser2 Nucleic Acids Res. 2024 May 8;52(8):4151-4166.
SaOS-2 osteosarcoma cells 10 μM 3 h BMH-9, BMH-22, and BMH-23 caused UBF cap formation, translocation of NCL from the nucleolus, and degradation of RPA194 in p53-null SaOS-2 cells, indicating that the nucleolar stress response is p53-independent. Mol Cancer Ther. 2014 Nov;13(11):2537-46
A375 melanoma cells 10 μM 3 h BMH-9, BMH-22, and BMH-23 significantly inhibited 5-FUrd incorporation and synthesis of the 45S precursor rRNA. Mol Cancer Ther. 2014 Nov;13(11):2537-46
MCF10A cells 1 µM 1 hour Inhibits RNA polymerase I transcriptional activity, leading to reduced nucleolar rRNA biogenesis Open Biol. 2022 Jan;12(1):210305
Yeast cells 300 nM 5 min BMH-21 disrupts Pol I's ability to clear the rDNA promoter, resulting in a 49% reduction in full-length RNA. J Biol Chem. 2022 Jan;298(1):101450

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Athymic NCr nu/nu mice Human melanoma and colon cancer xenograft models Intraperitoneal injection 25 mg/kg and 50 mg/kg 6 days on, one day off (A375) or daily (HCT116) To evaluate the antitumor activity of BMH-21 in vivo, results showed that BMH-21 significantly inhibited tumor growth. Cancer Cell. 2014 Jan 13;25(1):77-90

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.77mL

0.55mL

0.28mL

13.87mL

2.77mL

1.39mL

27.75mL

5.55mL

2.77mL

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