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530535 | RPA Inhibitor, TDRL-505 - Calbiochem

530535
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₄H₂₁BrClN₃O₄

      Pricing & Availability

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      5.30535.0001
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          Glass bottle 25 mg
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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
          FormOff-white solid
          Hill FormulaC₂₄H₂₁BrClN₃O₄
          Chemical formulaC₂₄H₂₁BrClN₃O₄
          ReversibleY
          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

          Documentation

          References

          Reference overview
          Anciano Granadillo, V.J., et al. 2010. J. Nucleic Acids 2010, 304035.
          Shuck, S.C., and Turchi, J.J. 2010. Cancer Res. 70, 3189.
          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
          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
          Chemical formulaC₂₄H₂₁BrClN₃O₄
          Purity≥97% by HPLC
          SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
          Storage -20°C
          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.
          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.