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Submit ReviewGeldanamycin
说明： Selective Hsp90 inhibitor
化学名： 9,13-Dihydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-2-azabicyclo[16.3.1]docosa-4,6,10,18,21-pentaene-3,20,22-trione, 9-carbamate
纯度： ≥98% (HPLC)
生物活性 for Geldanamycin
Geldanamycin is a selectively inhibits heat shock protein 90 (Hsp90). Binds to the ATP site of Hsp90 (Kd = 1.2 μM) and inhibits its chaperone activity. Consequently inhibits activities of oncogenic kinases (e.g. src, Raf), p53 and steroid receptors. Demonstrates antiproliferative effect on breast cancer stem-like cells.
技术数据 for Geldanamycin
| 分子量 | 560.64 |
| 公式 | C29H40N2O9 |
| 储存 | Desiccate at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 30562-34-6 |
| PubChem ID | 13017912 |
| InChI Key | QTQAWLPCGQOSGP-PHLMVCJGSA-N |
| Smiles | O=C1C(OC)=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.
溶解性数据 for Geldanamycin
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 5.61 | 10 |
制备储备液 for Geldanamycin
以下数据基于产品分子量 560.64。 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 | 17.84 mL | 89.18 mL | 178.37 mL |
| 0.5 mM | 3.57 mL | 17.84 mL | 35.67 mL |
| 1 mM | 1.78 mL | 8.92 mL | 17.84 mL |
| 5 mM | 0.36 mL | 1.78 mL | 3.57 mL |
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产品说明书 for Geldanamycin
参考文献 for Geldanamycin
参考文献是支持产品生物活性的出版物。
Cardenas et al (1998) Signal-transduction cascades as targets for therapeutic intervention by natural products. Trends Biotechnol. 16 427 PMID: 9807840
Roe et al (1999) Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanomycin. J.Med.Chem. 42 260 PMID: 9925731
Whitesell et al (1994) Inhibition of heat shock protein HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: essential role for stress proteins in oncogenic transformation. Proc.Natl.Acad.Sci.U.S.A. 91 8324 PMID: 8078881
Lee et al (2012) Inhibition of heat shock protein (Hsp) 27 potentiates the suppressive effect of Hsp90 inhibitors in targeting breast cancer stem-like cells. Biochimie. 94 1382 PMID: 22445681
If you know of a relevant reference for Geldanamycin, please let us know.
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关键词: Geldanamycin, Geldanamycin supplier, Selective, Hsp90, inhibitors, inhibits, Heat, Shock, Protein, 90, antibiotics, Antibiotics, Stem, Cell, Signaling, Cancer, Cells, 1368, Tocris Bioscience
5 篇 Geldanamycin 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Geldanamycin 的部分引用包括：
Barker et al (2006) Inhibition of Hsp90 acts synergistically with topoisomerase II poisons to increase the apoptotic killing of cells due to an increase in topoisomerase II mediated DNA damage. Neuroscience 34 1148 PMID: 16504968
Young et al (2015) A novel mechanism of autophagic cell death in dystrophic muscle regulated by P2RX7 receptor large-pore formation and HSP90. BMC Dev Biol 11 113 PMID: 25700737
Chung-Davidson et al (2015) Hsp90 and hepatobiliary transformation during sea lamprey metamorphosis. Nucleic Acids Res 15 47 PMID: 26627605
Yang et al (2018) NudCL2 is an Hsp90 cochaperone to regulate sister chromatid cohesion by stabilizing cohesin subunits. Cell Mol Life Sci PMID: 30368549
Khalafalla et al (2017) P2X7 receptor antagonism prevents IL-1β release from salivary epithelial cells and reduces inflammation in a mouse model of autoimmune exocrinopathy. J Biol Chem 292 16626 PMID: 28798231
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Geldanamycin 的评论
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Good Hsp90 blocker.
By
Anonymous on 01/27/2023
分析类型： In Vitro
种属： Rat
细胞系/组织： Primary hippocampal neurons
The drug was incubated at 10 μM to inhibit Hsp90.
Geldanamycin was used in resistance experiments.
By
Anonymous on 02/27/2019
种属： Human
Geldanamycin was used in resistance experiments. We investigated the Hsp90 family protein (HtpG) of the organism that makes GdA, S. hygroscopicus.
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