530535 RPA Inhibitor, TDRL-505 - Calbiochem

530535
View Pricing & Availability

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₄H₂₁BrClN₃O₄

Pricing & Availability

Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
5.30535.0001
Retrieving availability...
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      Contact Customer Service

      Glass bottle 25 mg
      Retrieving price...
      Price could not be retrieved
      Minimum Quantity needs to be mulitiple of
      Upon Order Completion More Information
      You Saved ()
       
      Request Pricing
      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
      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

      Documentation

      RPA Inhibitor, TDRL-505 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      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.