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530535 RPA Inhibitor, TDRL-505 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₄H₂₁BrClN₃O₄

Products

Catalog NumberPackaging Qty/Pack
5.30535.0001 Glass bottle 25 mg
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
Global Trade Item Number
Catalog Number GTIN
5.30535.0001 04055977260861

Documentation

RPA Inhibitor, TDRL-505 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

RPA Inhibitor, TDRL-505 - Calbiochem Certificates of Analysis

TitleLot Number
530535

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 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.