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General description
A 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Replication Protein A
Reversible: yes
Target IC50: 12.9, 15.7 and 30.8 µ
Packaging
Packaged under inert gas
Preparation Note
Use only fresh DMSO for reconstitution.
Other Notes
Anciano Granadillo, V.J., et al. 2010. J. Nucleic Acids2010, 304035.
Shuck, S.C., and Turchi, J.J. 2010. Cancer Res.70, 3189.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥97% (HPLC) |
| Quality Segment | 100 |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | off-white |
| solubility | DMSO: 50 mg/mL |
| storage temp. | −20°C |
| SMILES string | CCOC1=CC2=NC(=C(C=C2C=C1)C3CC(=NN3C(=O)CCC(=O)O)C4=CC=C(C=C4)Br)Cl |
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¥ 12156.68
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¥ 2013.69
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