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RPA Inhibitor, TDRL-505-Calbiochem

产品编号:4083611
规格:A cell-permeable compound that targets human Replication Protein A (RPA) and inhibits its DNA-binding activity (IC50= 12.9 μM).
包装规格:25 MG
产品类别:进口试剂
品牌:Sigma-Aldrich
优惠价:立即咨询
产品价格
产品编号包装单位单价(元)国内现货国外库存询价单
408361125 MG2950
产品别名

RPA Inhibitor, TDRL-505-Calbiochem

Replication Protein A Inhibitor, Pot1 Inhibitor, Protection of Telemeres Protein 1 Inhibitor, TDRL505

基本信息
Empirical Formula【经验(实验)分子式】
C24H21BrClN3O4
Molecular weight
530.80
General description【一般描述】
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.
A 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.
Biochem/physiol Actions【生化/生理作用】
Cell permeable: yes
Target IC50: 12.9, 15.7 and 30.8 &micro
Primary Target
Replication Protein A
Reversible: yes
Warning【警告】
Toxicity: Standard Handling (A)
Reconstitution【重悬】
Use only fresh DMSO for reconstitution.
Other Notes【其他说明】
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【法律信息】
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
产品性质
Quality Level【质量水平】
100
Assay【测定】
≥97% (HPLC)
form【形式】
solid
manufacturer/tradename
Calbiochem®
storage condition【储存条件】
OK to freeze
protect from light
color【颜色】
off-white
solubility【溶解性】
DMSO: 50 mg/mL
storage temp.【储存温度】
−20℃
packaging【包装】
Packaged under inert gas
安全信息
Storage Class Code【储存分类代码】
11 - Combustible Solids
WGK
WGK 3
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