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Submit Review17-AAG is an inhibitor of heat shock protein 90 (Hsp90) chaperone activity, and an analog of geldanamycin (Cat. No. 1368). Subsequently inhibits the activity of oncogenic proteins such as p185erbB-2 (IC50 = 31 nM), N-ras, Ki-ras and c-Akt. Antitumor in vivo. Also protects neuroprogenitor cells against stress-induced apoptosis at low concentrations (10 nM) in vitro.
分子量 | 585.7 |
公式 | C31H43N3O8 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 75747-14-7 |
PubChem ID | 6440175 |
InChI Key | AYUNIORJHRXIBJ-HTLBVUBBSA-N |
Smiles | O=C1C(NCC=C)=C(C[C@@H](C)C[C@H](OC)[C@H](O)[C@@H](C)/C=C(C)/[C@H](OC(N)=O)[C@@H](OC)/C=C/C=C(C)/C2=O)C(C(N2)=C1)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 5.86 | 10 |
以下数据基于产品分子量 585.7。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 17.07 mL | 85.37 mL | 170.74 mL |
0.5 mM | 3.41 mL | 17.07 mL | 34.15 mL |
1 mM | 1.71 mL | 8.54 mL | 17.07 mL |
5 mM | 0.34 mL | 1.71 mL | 3.41 mL |
参考文献是支持产品生物活性的出版物。
Hostein et al (2001) Inhibition of signal transduction by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin results in cytostasis and apoptosis. Cancer Res. 61 4003 PMID: 11358818
Schnur et al (1995) Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives. J.Med.Chem. 38 3806 PMID: 7562911
Yang et al (2001) Disruption of the EF-2 kinase/Hsp90 protein complex: a possible mechanism to inhibit glioblastoma by geldanamycin. Cancer Res. 61 4010 PMID: 11358819
Wang et al (2011) Protection of murine neural progenitor cells by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin in the low nanomolar concentration range. J.Neurochem. 117 703 PMID: 21395580
If you know of a relevant reference for 17-AAG, please let us know.
关键词: 17-AAG, 17-AAG supplier, Selective, Hsp90, inhibitors, inhibits, Heat, Shock, Protein, 90, NSC330507, antibiotics, stem, cells, protects, neural, progenitors, neuorprogenitors, stress-induced, apoptosis, Geldanamycin, NSC, 330507, 17-(Allylamino)-17-demethoxygeldanamycin, Tanespimycin, Antibiotics, Stem, Cell, Signaling, 1515, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 17-AAG 的部分引用包括:
Donnelly et al (2014) HSF1 deficiency and impaired HSP90-dependent protein folding are hallmarks of aneuploid human cells. EMBO J 33 2374 PMID: 25205676
Hughes et al (2012) Pertuzumab Increases 17-AAG-Induced Degradation of ErbB2, and This Effect Is Further Increased by Combining Pertuzumab with trastu. Pharmaceuticals (Basel) 5 674 PMID: 24281706
Fang et al (2014) HSP90 regulates DNA repair via the interaction between XRCC1 and DNA polymerase β. Nat Commun 5 5513 PMID: 25423885
Sontake et al (2017) Hsp90 regulation of fibroblast activation in pulmonary fibrosis. JCI Insight 2 e91454 PMID: 28239659
Siebert et al (2019) Heat Shock Protein 90 as a Prognostic Marker and Therapeutic Target for Adrenocortical Carcinoma. Front Endocrinol (Lausanne) 10 487 PMID: 31379752
Truman et al (2015) Quantitative proteomics of the yeast Hsp70/Hsp90 interactomes during DNA damage reveal chaperone-dependent regulation of ribonucleotide reductase. J Proteomics 112 285 PMID: 25452130
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平均评分: 5 (基于 2 条评论。)
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The drug was incubated at 100 nM to inhibit Hsp90.
I used it to down regulate the expression of HSP90. I checked using an antibody for HSP70 and showed upregulation of HSP70 with 10nM of 17-AAG. Easy to use product with informative data sheet. Stable in solution for months.
This is highly cytotoxic to human microglia at a high concentration (>100nM) from our cell viability data. We also confirmed this using imaging.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
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