Luminespib
CAS No.: 747412-49-3
- Molecular Formula: C₂₆H₃₁N₃O₅
- Molecular Weight: 465.5 g/mol
Chemical type
- Hsp90 inhibitor
- Small molecule inhibitor
- Resorcinyl isoxazole amine
- Synthetic Hsp90 inhibitor
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
- 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
- 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
- Hsp90 inhibitor
- Induces apoptotic cell death in cancer cells (e.g., papillary thyroid carcinoma)
- Anti-cancer agent tested in phase I/II clinical trials
Classification by use
- Anticancer agents
- Radiosensitizers
- Molecular chaperone inhibitors
- Therapeutics for overcoming treatment resistance
- Anti-cancer agents targeting molecular chaperones
- Chemicals for inhibiting protein maturation in tumor cells
A trustworthy factory and manufacturer
- [Cite:1] Radiosensitization of HSF-1 Knockdown Lung Cancer Cells by Low Concentrations of Hsp90 Inhibitor NVP-AUY922, Cells, 2019, 8(10), 1166
- [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
