产品说明
一般描述
A cell-permeable, benzoquinone compound that exhibits anti-tumor properties. Shown to specifically antagonize X-linked inhibitor of apoptosis- (XIAP) mediated inhibition of caspase-9 activation by directly targeting the Smac and caspase-9 binding domain BIR3 (IC50 = 4.1 µM in a competitive binding assay using Smac peptide). Also selectively induces caspase-9-mediated apoptosis in prostate cancer cells expressing high levels of XIAP (IC50 = 3.7 µM for PC-3 cells and 5.7 µM for LnCap cells), while exhibiting lesser effects toward cells with low levels of XIAP (IC50 = 19.3 µM for WI-38 cells and 20.1 µM for PrEC cells). Reported to sensitize XIAP-overexpressing Jurkat cells to Etoposide- (Cat. No. 341245) induced apoptosis. A non-competitive PCAF (p300/CBP associated factor)-specific lysine acetyltransferase (KAT) inhibitor (IC50 = 7.2 µM).
A cell-permeable benzoquinone compound that exhibits antitumor properties. Specifically antagonizes XIAP (X-linked inhibitor of apoptosis)-mediated inhibition of caspase-9 activation by directly targeting the Smac and caspase-9 binding domain BIR3 (IC50 = 4.1 µM in a competitive binding assay with Smac peptide). Selectively induces caspase-9-mediated apoptosis in prostate cancer cells with high levels of XIAP (IC50 = 3.7 and 5.7 µM for PC-3 and LnCap, respectively), while exhibiting much less effect towards cells with low level XIAP (IC50 = 19.3 and 20.1 µM for WI-38 and PrEC, respectively). Also shown to sensitize XIAP overexpressing Jurkat cells to Etoposide -induced apoptosis. A non-competitive PCAF (p300/CBP associated factor)-specific lysine acetyltransferase (KAT) inhibitor (IC50 = 7.2 µM).
包装
10 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Primary Target
BIR3
Product does not compete with ATP.
Reversible: no
Target IC50: 4.1 µM in antagonizing XIAP (X-linked inhibitor of apoptosis)-mediated inhibition of caspase-9 activation by directly targeting the Smac and caspase-9 binding domain BIR3 in a competitive binding assay with Smac peptide
警告
Toxicity: Standard Handling (A)
分析说明
Single spot by TLC
其他说明
Modak, R., et al. 2013. ACS Chem. Biol.8, In press.
Nikolovska-Coleska, Z., et al. 2004. J. Med. Chem.47, 2430.
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 | C17H26O4 |
| 分子量 | 294.39 |
| MDL编号 | MFCD00016369 |
产品性质
| 质量水平 | 100 |
| 形式 | solid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze protect from light |
| 颜色 | orange |
| 溶解性 | DMSO: 10 mg/mL methanol: 5 mg/mL |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
| InChI | 1S/C17H26O4/c1-2-3-4-5-6-7-8-9-10-11-13-16(20)14(18)12-15(19)17(13)21/h12,18,21H,2-11H2,1H3 |
| InChI key | IRSFLDGTOHBADP-UHFFFAOYSA-N |
安全信息
| 象形图 |  |
| 警示用语： | Warning |
| 危险声明 | H361f |
| 预防措施声明 | P201 - P202 - P280 - P308 + P313 - P405 - P501 |
| 危险分类 | Repr. 2 |
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
