747412-49-3 | NVP-AUY922

Chemical type

• Hsp90 inhibitor
• Small molecule inhibitor

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• Resorcinyl isoxazole amine
• Synthetic Hsp90 inhibitor

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Key properties

• Potent and selective inhibitor of Hsp90
• Induces release and activation of HSF-1, leading to upregulation of cytoprotective proteins Hsp70 and Hsp27 at higher concentrations
• Reduces expression of Hsp90 client proteins such as Akt
• Impairs DNA double-strand break repair, particularly homologous recombination mediated by Rad51
• Less toxic than earlier Hsp90 inhibitors, with improved biodistribution
• Promising anti-tumor activity in vitro, including radiosensitization effects
• Effective at low concentrations (1-10 nM) when combined with HSF-1 knockdown, minimizing adverse induction of stress proteins

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• ATP-competitive binder to N-terminal domain
• IC50 of 13 nM for Hsp90α and 21 nM for Hsp90β
• High affinity in tumor cells (100-fold higher than in normal cells)
• Stable in ATP pocket with binding free energy of -49.4 kcal/mol
• Induces cleavage of PARP and caspase-3, alters survivin expression

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• Radiosensitizer for lung cancer cells, enhancing radiation-induced cell death and DNA damage
• Combined with HSF-1 knockdown to potentiate effects on radioresistant tumors
• Potential therapeutic agent to overcome radio- and chemoresistance in cancers
• Inhibits tumor growth, angiogenesis, and metastasis in preclinical models
• Evaluated for clinical applications, with reduced hepatotoxic side effects compared to high-dose regimens

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• Hsp90 inhibitor
• Induces apoptotic cell death in cancer cells (e.g., papillary thyroid carcinoma)
• Anti-cancer agent tested in phase I/II clinical trials

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Classification by use

• Anticancer agents
• Radiosensitizers
• Molecular chaperone inhibitors
• Therapeutics for overcoming treatment resistance

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• Anti-cancer agents targeting molecular chaperones
• Chemicals for inhibiting protein maturation in tumor cells

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A trustworthy factory and manufacturer

Demei Chemical Technology Co., Ltd. is a modern high-tech enterprise integrating R&D, production, and sales. The company's founder, Dr. Arron, born in April 1975, graduated from the School of Mechanical Engineering at Yanshan University and has been engaged in research in the fields of mechanical engineering and chemical synthesis for many years. The company's products focus on the chemical industry, primarily dealing in chemical raw materials and chemical production machinery and equipment. With its strong technical capabilities, advanced production equipment, and strict quality management system, the company has earned the trust of customers worldwide.

1. [Cite:1] Radiosensitization of HSF-1 Knockdown Lung Cancer Cells by Low Concentrations of Hsp90 Inhibitor NVP-AUY922, Cells, 2019, 8(10), 1166
2. [Cite:2] Exploring the inhibitory mechanism of resorcinylic isoxazole amine NVP-AUY922 towards the discovery of potential heat shock protein 90 (Hsp90) inhibitors, Scientific African, Volume 15, March 2022, e01107