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BMH-21

Catalog No. T1767 CAS 896705-16-1

Synonyms: BMH21

BMH-21, a small molecule DNA intercalator, binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription and not affects phosphorylation of H2AX.

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BMH-21, CAS 896705-16-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 35.00
10 mg	In stock	$ 56.00
25 mg	In stock	$ 98.00
50 mg	In stock	$ 166.00
100 mg	In stock	$ 288.00
200 mg	In stock	$ 432.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.53%

Purity: 99.47%

Purity: 98.87%

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Description	BMH-21, a small molecule DNA intercalator, binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription and not affects phosphorylation of H2AX.
Targets&IC50	RNA polymerase I:10-90 nM
In vitro	In xenograft models using mice, BMH-21 can inhibit tumor growth.
In vivo	In the U2OS cancer cell line, BMH-21 induces the translocation of NCL (IC50: 0.07 μM) and the degradation of RPA194 (IC50: 0.05 μM). BMH-21 triggers proteasomal destruction dependent on RPA194, where RPA194 is the large catalytic subunit protein of the Pol I complex. By inducing nucleolar stress, BMH-21 also effectively inhibits cellular activity.
Kinase Assay	[14C]-monosaccharide uptake inhibition experiments: Stable cell lines over-expressing hSGLT-1, -2, -4, -5 or -6 or rSGLT-1 or -2 are used for the sodium-dependent monosaccharide transport inhibition assay. Cells are pre-incubated in 200 μL uptake buffer (10 mM HEPES, 137 mM NaCl, 5.4 mM KCl, 2.8 mM CaCl2, 1.2 mM MgCl2, 50 μg/ml Gentamycin, 0.1% BSA) for 25 minutes at 37°C. 10 μM Cytochalasin B and test compound is added at different concentrations 15 minutes before the initiation of the uptake experiment. The uptake reaction is started by the addition of 0.6 μCi [14C]-labelled monosaccharide i.e. [14C]-labelled AMG, glucose, fructose, mannose or myo-inositol, in 0.1 mM AMG (or the respective non-radioactive monosaccharide). After incubation for 60 minutes (hSGLT-5), 90 minutes (hSGLT-4) or 4 hours (hSGLT-2) at 37°C, the cells are washed three times with 300 μL PBS and then lysed in 0.1 N NaOH with intermittent shaking for 5 minutes. The lysate is mixed with 200 μL MicroScint 40 and shaken for 15 minutes and counted for radioactivity in the TopCount NXT. For SGLT-4 and SGLT-5 assays cells are pre-incubated in pre-treatment buffer (uptake buffer containing choline chloride instead of NaCl) for 25 minutes prior to addition of uptake buffer.
Cell Research	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. (Only for Reference)

Synonyms	BMH21
Molecular Weight	360.41
Formula	C21H20N4O2
CAS No.	896705-16-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 2 mg/mL (5.54 mM), Heating is recommended.

DMSO: 5 mg/mL (13.87 mM), Heating is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Peltonen K, et al. Cancer Cell. 2014, 25(1), 77-90. 2. Colis L, et al. J Med Chem. 2014, 57(11), 4950-4961.

Citations

1. Scalera, Claudia, et al. Transcriptional Stress Induces Chromatin Relocation of the Nucleotide Excision Repair Factor XPG. International Journal of Molecular Sciences. 22.12 (2021): 6589.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library CNS-Penetrant Compound Library Target-Focused Phenotypic Screening Library Bioactive Compounds Library Max Cell Cycle Compound Library Anti-Aging Compound Library Bioactive Compound Library DNA Damage & Repair Compound Library Immunology/Inflammation Compound Library

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Keywords

BMH-21 896705-16-1 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis nucleolus polymerase damage intercalation transcription RNA BMH 21 response DNA BMH21 inhibit Inhibitor inhibitor

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