| 产品描述： | The Hsp90 family of molecular chaperones regulates and maintains cell homeostasis under proteotoxic stress and pathogenic pressure. In humans, Hsp90α and Hsp90β in the cytoplasm, Grp94 in the endoplasmic reticulum and Trap-1 in the mitochondria are the four Hsp90 paralogs. PU-WS13 is a potent, Grp94-specific Hsp90 inhibitor of the purine scaffold class |
| 靶点： |
Estrogen/progestogenReceptor |
| 体外研究： |
Brief treatment of SKBr3 cells with PU-WS13 disrupted the circular architecture of HER2 at the plasma membrane, resulting in a ‘shredded’ HER2 pattern. The effect of PU-WS13 on the HER2 surface architecture is mediated through Grp94. Upon treatment of cells with PU-WS13, a rapid accumulation of cells in the sub-G1 phase, PARP cleavage and a substantial increase in markers of early- and late-stage apoptosis were noted |
| 体内研究： |
Potent and durable anti-tumor effects in TNBC xenografts, including complete response and tumor regression, without toxicity to the host are achieved with PUH71, a chemical analogue of PU-WS13. Notably, TNBC tumors respond to retreatment with PUH71 for several cycles extending for over 5 months without evidence of resistance or toxicity |
| 细胞实验： |
Cells are treated for 72 h with inhibitors (including PU-WS13) or transfected with Grp94 siRNA or control siRNA, and their viability is assessed using CellTiter-Glo luminescent Cell Viability Assay. The method determines the number of viable cells in culture based on quantification of the ATP present, which signals the presence of metabolically active cells |
| 参考文献： |
1. Patel PD, Yan P, Seidler PM, Patel HJ, Sun W, Yang C, Que NS, Taldone T, Finotti P, Stephani RA, Gewirth DT, Chiosis G. Paralog-selective Hsp90 inhibitors define tumor-specific regulation of HER2. Nat Chem Biol. 2013 Nov;9(11):677-84. 2. Caldas-Lopes E, Cerchietti L, Ahn JH, Clement CC, Robles AI, Rodina A, Moulick K, Taldone T, Gozman A, Guo Y, Wu N, de Stanchina E, White J, Gross SS, Ma Y, Varticovski L, Melnick A, Chiosis G. Hsp90 inhibitor PU-H71, a multimodal inhibitor of malignancy, induces complete responses in triple-negative breast cancer models. Proc Natl Acad Sci U S A. 2009 May 19;106(20):8368-73. 3. Patel PD, et al. Paralog-selective Hsp90 inhibitors define tumor-specific regulation of HER2. Nat Chem Biol. 2013 Nov;9(11):677-684. |
| 溶解性： |
Soluble in DMSO、Ethanol、DMF |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.431 ml |
12.155 ml |
24.31 ml |
| 5 mM |
0.486 ml |
2.431 ml |
4.862 ml |
| 10 mM |
0.243 ml |
1.216 ml |
2.431 ml |
| 50 mM |
0.049 ml |
0.243 ml |
0.486 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京