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530535 RPA Inhibitor, TDRL-505 - CAS 1785760-75-9 - Calbiochem

A cell-permeable compound that targets human Replication Protein A (RPA) and inhibits its DNA-binding activity (IC₅₀= 12.9 µM).

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: Replication Protein A Inhibitor, Pot1 Inhibitor, Protection of Telemeres Protein 1 Inhibitor, TDRL505

Primary Target: Replication Protein A
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530535
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Tableau de caractéristiques principal

CAS #Empirical Formula
1785760-75-9C₂₄H₂₁BrClN₃O₄

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      Description
      OverviewA cell-permeable quinolinyl-dihydropyrazolyl-oxobutanoic acid compound that is shown to target human Replication Protein A (RPA) via primarily the oligosaccharide/oligonucleotide-binding (OB) folds of DNA-bonding domains A & B (DBD-A/B) in the p70 subunit, effectively inhibiting its DNA-binding activity as well as that of Schizosaccharomyces pombe telemere end-binding protein Pot1 (IC50= 12.9 µM and 15.7 µM, respectively), but not Xeroderma pigmentosum group A protein (XPA) involved in the nucleotide excision repair (NER) pathway or E. coli SSB. Reported to induce cell cycle G1-arrest and decrease Annvex V-/PI- healthy cell population (by 50%; 30.8 µM for 48 h) in H460 non-small cell lung carcinoma (NSCLC) cultures with minimal cytotoxicity against freshly isolated human PBMC. Potentiates cisplatin (Cat. No. 232120) and etopside (Cat. No. 341205) cytotoxicity in H460 cultures in a synergistic manner.
      Catalogue Number530535
      Brand Family Calbiochem®
      SynonymsReplication Protein A Inhibitor, Pot1 Inhibitor, Protection of Telemeres Protein 1 Inhibitor, TDRL505
      References
      ReferencesAnciano Granadillo, V.J., et al. 2010. J. Nucleic Acids 2010, 304035.
      Shuck, S.C., and Turchi, J.J. 2010. Cancer Res. 70, 3189.
      Product Information
      CAS number1785760-75-9
      FormOff-white solid
      Hill FormulaC₂₄H₂₁BrClN₃O₄
      Chemical formulaC₂₄H₂₁BrClN₃O₄
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetReplication Protein A
      Primary Target IC<sub>50</sub>12.9, 15.7 and 30.8 µ
      Purity≥97% 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 -20°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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      5.30535.0001 04055977260861

      Documentation

      RPA Inhibitor, TDRL-505 - CAS 1785760-75-9 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      RPA Inhibitor, TDRL-505 - CAS 1785760-75-9 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      530535

      Références bibliographiques

      Aperçu de la référence bibliographique
      Anciano Granadillo, V.J., et al. 2010. J. Nucleic Acids 2010, 304035.
      Shuck, S.C., and Turchi, J.J. 2010. Cancer Res. 70, 3189.
      Fiche technique

      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
      SynonymsReplication Protein A Inhibitor, Pot1 Inhibitor, Protection of Telemeres Protein 1 Inhibitor, TDRL505
      DescriptionA cell-permeable quinolinyl-dihydropyrazolyl-oxobutanoic acid compound that is shown to target human Replication Protein A via primarily the oligosaccharide/oligonucleotide-binding (OB) folds of DNA-bonding domains A & B (DBD-A/B) in the p70 subunit, effectively inhibiting its DNA-binding activity as well as that of Schizosaccharomyces pombe telemere end-binding protein Pot1 (IC50= 12.9 µM/25 nM hRPA/25 nM 34-base AG-rich ssDNA and 15.7 µM/20 nM SpPot1 DBD/25 nM 15-base ssDNA), but not Xeroderma pigmentosum group A protein (XPA) involved in the nucleotide excision repair (NER) pathway or E. coli SSB (20% inhibition at 100 µM against 3.3 nM EcSSB & 25 nM 3Pc3 ssDNA binding). Reported to cause decreased nuclear RPA staining (50 µM for 3 h), cell cycle G1-arrest (75 to 100 µM), and a drop in Annvex V-/PI- healthy cell population (by 50%; 30.8 µM for 48 h) in H460 non-small cell lung carcinoma (NSCLC) cultures with minimal cytotoxicity against freshly isolated human PBMC. Potentiates cisplatin (Cat. No. 232120) and etopside (Cat. No. 341205) cytotoxicity in H460 cultures in a synergistic manner, consistent with blockage of RPA-mediated NER pathway.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1785760-75-9
      Chemical formulaC₂₄H₂₁BrClN₃O₄
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
      Storage Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesAnciano Granadillo, V.J., et al. 2010. J. Nucleic Acids 2010, 304035.
      Shuck, S.C., and Turchi, J.J. 2010. Cancer Res. 70, 3189.