5.30535

RPA Inhibitor, TDRL-505

• 別名: RPA Inhibitor, TDRL-505, Replication Protein A Inhibitor, Pot1 Inhibitor, Protection of Telemeres Protein 1 Inhibitor, TDRL505
• 実験式（ヒル表記法）: C₂₄H₂₁BrClN₃O₄
• CAS番号: 1785760-75-9
• 分子量: 530.80
• UNSPSCコード: 12352200
• PubChem Substance ID: 5212392
• NACRES: NA.77

特性

• アッセイ: ≥97% (HPLC)
• 品質水準: 100
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: off-white
• 溶解性: DMSO: 50 mg/mL
• 保管温度: −20°C
• SMILES記法: CCOC1=CC2=NC(=C(C=C2C=C1)C3CC(=NN3C(=O)CCC(=O)O)C4=CC=C(C=C4)Br)Cl

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
Replication Protein A

Reversible: yes

Target IC₅₀: 12.9, 15.7 and 30.8 &micro

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Use only fresh DMSO for reconstitution.

その他情報

Anciano Granadillo, V.J., et al. 2010. J. Nucleic Acids2010, 304035.

Shuck, S.C., and Turchi, J.J. 2010. Cancer Res.70, 3189.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable