Luminespib

SKU: orb1306830

Description

Luminespib (VER-52296) is a potent and selective HSP90 inhibitor targeting both HSP90α and HSP90β isoforms. It demonstrates significant antitumor activity in preclinical studies, including in vitro cell-based assays and in vivo models for head and neck squamous cell carcinoma and other malignancies.

Research Area

Cell Biology, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 747412-49-3
• MW: 465.54
• Purity: 99.26% (May vary between batches)
• Formula: C₂₆H₃₁N₃O₅
• SMILES: CCNC(=O)c1noc(c1-c1ccc(CN2CCOCC2)cc1)-c1cc(C(C)C)c(O)cc1O
• Target: Apoptosis,Autophagy,HSP
• Solubility: DMSO:16.67 mg/mL (35.81 mM);Ethanol:29 mg/mL (62.29 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:8.6 mg/mL (18.47 mM)

Bioactivity

• Target IC50:
  HSP90 α:7.8 nM (cell free)|TRAP1:85 nM|HSP90 β:21 nM (cell free)|GRP94:535 nM
• In Vivo:
  METHODS: To study the effect on H. pylori-associated gastritis, Patchouli alcohol (5-20 mg/kg) was administered orally to H. pylori infected mice once daily for two weeks. RESULTS: Patchouli alcohol treatment increased SH-NP content and CAT activity and significantly protected the gastric mucosa from H. pylori-induced damage.
• In Vitro:
  METHODS: H. pylori infected GES-1 cells were treated with Patchouli alcohol (5-20 µg/mL) for 24 h. Apoptosis was detected by flow cytometry. RESULTS: Patchouli alcohol treatment significantly reduced H. pylori-induced apoptosis. METHODS: H. pylori-infected GES-1 cells were treated with Patchouli alcohol (5-20 µg/mL) for 24 h. Cytokine levels were measured by ELISA. RESULTS: Treatment with 5-20 µg/mL Patchouli alcohol significantly reduced the production of TNF-α and MCP-1.
• Cell Research:
  Cell lines were grown in DMEM/10% FCS, 2 mmol/L glutamine, and nonessential amino acids in a humidified atmosphere of 5% CO2 in air. All lines were free of Mycoplasma. Cell proliferation was determined using the sulforhodamine B (SRB) assay for tumor cells and prostate epithelial cells, the WST-1 assay for MCF10A and HB119, or an alkaline phosphatase assay for HUVEC and HDMEC. GI50 was the compound concentration inhibiting cell proliferation by 50% compared with vehicle controls. Cell cycle analysis was as described. Active caspase-3/7 was measured using a homogenous caspase assay kit .
• Animal Research:
  In vivo, pharmacokinetic studies in female NCr athymic mice bearing WM266.4 human melanoma xenografts were essentially as described. NVP-AUY922 was dissolved in DMSO and diluted in sterile saline/Tween 20. A single dose of 50 mg/kg NVP-AUY922 was given i.v. or i.p. and groups of three animals were taken at intervals for pharmacokinetic analyses .

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NVP-AUY 922, NVP-AUY922, NVP-AUY-922, Luminespib, inhibit, Inhibitor, Heat shock proteins, HSP, HSP90β, HSP90α, Autophagy, AUY 922, AUY922, AUY-922, Apoptosis, VER52296, VER-52296, VER 52296

Structure of Luminespib.

Compound Identifiers

PubChem CID

135539077

Mohammed Fulayyih Aloufi et al. Luminespib protects against dexamethasone-induced hepatic, vascular, and metabolic abnormalities in rats Naunyn Schmiedebergs Arch Pharmacol, (2025)

PubMed: 41273382