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509911 RNA Polymerase I Inhibitor II, BMH-21 - CAS 896705-16-1 - Calbiochem

A cell-permeable compound that blocks the growth and viability of a variety of cancer cell lines (GI₅₀ = 160 nM in NCI-60 cells), but does not affect normal cells.

RNA Polymerase I Inhibitor II, BMH-21 - CAS 896705-16-1 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-(2-(Dimethylamino)ethyl)-12-oxo-12H-benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide, BMH21, rRNA Transcription Inhibitor II

Primary Target: rDNA
509911
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
896705-16-1C₂₁H₂₀N₄O₂

Products

Catalogue NumberPackaging Qty/Pack
5.09911.0001 Sklená flaša 10 mg
Description
OverviewA cell-permeable, non-toxic, benzopyridoquinazoline-carboxamide compound that blocks the growth and viability of a variety of cancer cell lines (GI50 = 160 nM in NCI-60 cells), but does not significantly affect normal cells (~90-fold therapeutic window). Preferentially binds to the GC-rich DNA and inhibits RNA polymerase I (Pol I) transcription. Although it intercalates with DNA, it does not activate the DNA damage response. Induces a proteasome-dependent destruction of large Pol I catalytic subunit RPA194, independent of TP53 genetic status of cancer cells, leading to disassembly of Pol I holocomplex from the rDNA. However, it does not affect Rpb1, the large subunit of RNA polymerase II and Pol I preinitiation complex proteins. Effectively reduces the growth of A375 and HCT116 xenografts in athymic NCr nu/nu mice (50 mg/kg, i.p, 2 weeks).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number509911
Brand Family Calbiochem®
SynonymsN-(2-(Dimethylamino)ethyl)-12-oxo-12H-benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide, BMH21, rRNA Transcription Inhibitor II
References
ReferencesPeltonen, K., et al. 2014. Cancer Cell 25, 77.
Peltonen, K., et al. 2010. PLoS One 5, e12996.
Product Information
CAS number896705-16-1
FormOrange-yellow powder
Hill FormulaC₂₁H₂₀N₄O₂
Chemical formulaC₂₁H₂₀N₄O₂
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetrDNA
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
5.09911.0001 04055977241181

Documentation

RNA Polymerase I Inhibitor II, BMH-21 - CAS 896705-16-1 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Peltonen, K., et al. 2014. Cancer Cell 25, 77.
Peltonen, K., et al. 2010. PLoS One 5, e12996.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision04-June-2014 JSW
SynonymsN-(2-(Dimethylamino)ethyl)-12-oxo-12H-benzo[g]pyrido[2,1-b]quinazoline-4-carboxamide, BMH21, rRNA Transcription Inhibitor II
DescriptionA cell-permeable, reversible DNA-intercalating benzopyridoquinazoline-carboxamide that preferentially targets GC-rich sequence, notably that of rDNA (162% of average human genome GC content), and effectively inhibits RNA polymerase I- (Pol I) mediated rDNA transcription both in cell-free assays and in cultures (IC50/ICmax = 60 nM/≤1 µM against 2-h de novo 47S transcription in A375 cells) without affecting the maturation/processing of 47S into 32S and 18S rRNA. Time-dependent studies in 1 µM BMH-21-treated A375 cells reveal fast inhibition of nuclear RNA synthesis (FUrd incorporation) within 15 min, followed by progressive altered localization of nucleolar proteins (starting in <20 min), including Pol I subunit RPA194 capping structure formation, indicative of stalled Pol I complex, and eventual proteasome-mediated RPA194 degradation (>1 h). Although BMH-21 activates p53 independent of DNA damage-sensing ATM pathway signaling in A375 cultures, wt p53 is not a prerequisite for BMH-21 anticancer activity (Av GI50 = 110 nM/wt and 205 nM/mutant among NCI60 cancer panel). Intraperitoneal injection is demonstrated to be efficacious in suppressing A375 (25 & 50 mg/kg/d, 6d/wk) and HCT-116 (50 mg/kg/d, 7 d/wk) tumor growth in mice in vivo. MG-132 (Cat. Nos. 474790, 474787, 474788, and 474791) effectively prevents BMH-21-induced RPA194 degradation without restoring stalled rRNA synthesis.
FormOrange-yellow powder
Intert gas (Yes/No) Packaged under inert gas
CAS number896705-16-1
Chemical formulaC₂₁H₂₀N₄O₂
Purity≥98% by HPLC
SolubilityDMSO (1 mg/ml) or 5% Aqueous Acetic Acid (25 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesPeltonen, K., et al. 2014. Cancer Cell 25, 77.
Peltonen, K., et al. 2010. PLoS One 5, e12996.