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HSP90(热休克蛋白90 kDa)是热休克蛋白(HSP)家族的成员。热休克蛋白属于伴侣蛋白,其功能包括帮助蛋白质正确折叠、抵抗热应激相关压力、通过作用于激素受体和激酶参与细胞信号传导、参与细胞骨架组织、通过作用于细胞周期蛋白依赖性激酶4(CDK4)、Wee1和CDK11p110等参与细胞周期和分化等。HSP90有三个家族成员,它们的细胞定位不同。HSP90A是一种胞质蛋白,有两种诱导型异构体(HSP90α1和α2)以及一种组成型表达的异构体(HSP90β)。胞质HSP90作为伴侣蛋白,可防止蛋白质聚集,还参与细胞信号传导、DNA结构维持、细胞周期调控以及细胞骨架稳定。由于胞质HSP90的客户蛋白中包含与癌症相关的因子,因此它成为这种疾病中的一种重要蛋白。在许多癌症中都发现了HSP90的高表达,这一现象被称为“伴侣蛋白增加”,即突变蛋白产生增多时,需要更多的伴侣蛋白。因此,HSP90已成为癌症治疗中一个极具吸引力的治疗靶点。除癌症外,HSP90还可能在阿尔茨海默病、帕金森病和病毒感染中发挥作用。显然,鉴于其多种关键功能,开发靶向HSP90的抑制剂可能对多种使人衰弱的致命疾病的治疗有益。
N端HSP90α格尔德霉素竞争性抑制剂检测试剂盒是一种竞争性荧光偏振(FP)均相检测试剂盒,旨在测量HSP90α(热休克蛋白90α)的N端区域与含有HSP90抑制剂格尔德霉素的荧光探针之间复合物的形成。当探针与HSP90α结合时,荧光偏振值较高。若存在一种受试化合物,其能与格尔德霉素结合到HSP90α上的相同位点,则含格尔德霉素的荧光探针会从HSP90α上被置换下来并留在溶液中,导致荧光偏振值降低。该试剂盒采用便捷的384孔板格式,包含足够的纯化重组HSP90α酶、FITC标记的格尔德霉素以及HSP90检测缓冲液,可进行400次酶反应。
HSP90α与含格尔德霉素的荧光探针结合,形成复合物。该复合物在受到偏振激发光照射时,由于其在溶液中的运动受限,会发出高偏振光。在存在测试抑制剂的情况下,HSP90α可能与测试抑制剂形成复合物(如果测试抑制剂与格尔德霉素在HSP90α上具有相同的结合位点),也可能与含格尔德霉素的荧光探针形成复合物。如果测试化合物与HSP90α的同一位点结合,含格尔德霉素的荧光探针就会被释放,此时可观察到荧光偏振(FP)降低。FP值的降低与测试化合物对HSP90α的竞争性结合成正比。
Target(s)
HSP90a
UniProt #
P07900
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产品组分
内容 型号
规格 储存温度
N端HSP90α格尔德霉素竞争性抑制剂检测试剂盒
50298-01 384次
-20°C N端HSP90α格尔德霉素竞争性抑制剂检测试剂盒
50298-02 768次
-20°C 操作手册
1 1 常温
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注意事项
保存建议 厂家推荐蓝冰运输。当您收到产品后,按照说明书建议保存于-20°C。 -
FAQ
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References
Kim J., et al., 2004 Biomol. Screening 9(5): 375-381.
Howes R., et al., 2006 Anal. Biochem. 350:202-213.
Hoter A., et al., 2018 Int J Mol Sci. 19(9):2560.
New Class of Hsp90 C-Terminal Domain Inhibitors with Anti-tumor Properties against Triple-Negative Breast Cancer.
Živa Zajec, Jaka Dernovšek, ..., Tihomir Tomašič
Journal of Medicinal Chemistry | 2024 Jul 23 | 39042910
The HDAC/HSP90 Inhibitor G570 Attenuated Blue Light-Induced Cell Migration in RPE Cells and Neovascularization in Mice through Decreased VEGF Production
Tai-Ju Hsu, Kunal Nepali, ..., Yu-Wen Cheng
Molecules | 2021 Jul 19
Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo
Yi-Min Liu, Huang-Ju Tu, ..., Jing-Ping Liou
European Journal of Medicinal Chemistry | 2021 Jul 01 | 33934008
Elaiophylin Is a Potent Hsp90/ Cdc37 Protein Interface Inhibitor with K-Ras Nanocluster Selectivity
Farid A. Siddiqui, Vladimir Vukic, ..., Vladimir N. Uversky
Biomolecules | 2021 Jun 04 | 34199986
Novel Small Molecule Hsp90/Cdc37 Interface Inhibitors Indirectly Target K-Ras-Signaling
Farid Ahmad Siddiqui, Hanna Parkkola, ..., Anupama Munshi
Cancers | 2021 Feb 23 | 33672199
Amide-tethered quinoline-resorcinol conjugates as a new class of HSP90 inhibitors suppressing the growth of prostate cancer cells.
Kunal Nepali, Mei-Hsiang Lin, ..., Jing-Ping Liou
Bioorganic Chemistry | 2020 Oct 21 | 31349117
N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression.
Samir Mehndiratta, Mei-Hsiang Lin, ..., Jing-Ping Liou
European Journal of Medicinal Chemistry | 2020 Feb 18 | 31655430
Rational Design of Selective Adenine-Based Scaffolds for Inactivation of Bacterial Histidine Kinases
Manibarsha Goswami, Kaelyn E. Wilke, Erin E. Carlson
Journal of Medicinal Chemistry | 2018 Oct 12 | 28933546
Patent Methods of treating a metabolic syndrome by modulating heat shock protein (HSP) 90-beta
Niven Rajin Narain, Rangaprasad Sarangarajan, ..., Enxuan Jing
us10023864 | 2018 Jul 17
Patent Methods of treating a metabolic syndrome by modulating heat shock protein (HSP) 90-β
Niven Rajin Narain, Rangaprasad Sarangarajan, ..., Enxuan Jing
us09533002 | 2017 Jan 03
Disruption of Heat Shock Protein 90 (Hsp90)-Protein Kinase Cδ (PKCδ) Interaction by (−)-Maackiain Suppresses Histamine H 1 Receptor Gene Transcription in HeLa Cells
Yuki Nariai, Hiroyuki Mizuguchi, ..., Hiroyuki Fukui
The Journal of Biological Chemistry | 2015 Sep 21 | 26391399
The Quinone Methide Aurin Is a Heat Shock Response Inducer That Causes Proteotoxic Stress and Noxa-dependent Apoptosis in Malignant Melanoma Cells
Angela L. Davis, Shuxi Qiao, ..., Georg T. Wondrak
The Journal of Biological Chemistry | 2015 Jan 16 | 25477506
Herbimycins D-F, Ansamycin Analogues from Streptomyces sp. RM-7-15
Khaled A Shaaban, Xiachang Wang, ..., Jon S Thorson
Journal of Natural Products | 2013 Sep 27 | 23947794
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