半岛bd体育手机客户端 说明
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 ofSchizosaccharomyces pombetelemere end-binding protein Pot1 (IC50= 12.9 ?M/25 nM hRPA/25 nM 34-base AG-rich ssDNA and 15.7 ?M/20 nMSpPot1 DBD/25 nM 15-base ssDNA), but not Xeroderma pigmentosum group A protein (XPA) involved in the nucleotide excision repair (NER) pathway orE. coliSSB (20% inhibition at 100 ?M against 3.3 nMEcSSB & 25 nM 3Pc3 ssDNA binding). Reported to cause decreased nuclear RPA staining (50 ?M for 3 h), cell cycle G1-arrest (75 to 100 ?M), and a drop in Annvex V-/PI-healthy cell population (by 50%; 30.8 ?M 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 ofSchizosaccharomyces pombetelemere end-binding protein Pot1 (IC50= 12.9 ?M and 15.7 ?M, respectively), but not Xeroderma pigmentosum group A protein (XPA) involved in the nucleotide excision repair (NER) pathway orE. coliSSB. Reported to induce cell cycle G1-arrest and decrease Annvex V-/PI-healthy cell population (by 50%; 30.8 ?M 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.
生化/生理作用
Cell permeable: yes
Target IC50: 12.9, 15.7 and 30.8 µ
Primary Target
Replication Protein A
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Use only fresh DMSO for reconstitution.
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C24H21BrClN3O4 |
| 分子量 | 530.80 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥97% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze protect from light |
| 颜色 | off-white |
| 溶解性 | DMSO: 50 mg/mL |
| 储存温度 | ?20℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
