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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.

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

Primary Target: rDNA
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509911
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Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
896705-16-1C₂₁H₂₀N₄O₂

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      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
      Bestellnummer GTIN
      5099110001 04055977241181

      Documentation

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

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Peltonen, K., et al. 2014. Cancer Cell 25, 77.
      Peltonen, K., et al. 2010. PLoS One 5, e12996.
      Datenblatt

      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.