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

Cardiovascular Research, Cell Biology, Immunology & Inflammation

Key Properties

• CAS Number: 747412-49-3
• MW: 465.5
• Purity: >99%
• Formula: C₂₆H₃₁N₃O₅
• SMILES: CCNC(=O)c1noc(c1-c1ccc(CN2CCOCC2)cc1)-c1cc(C(C)C)c(O)cc1O
• Target: HSP (Heat shock protein)
• Solubility: Soluble in DMSO (up to 25 mg/ml)

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.
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• 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.
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• 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 .
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• 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 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NVP-AUY922; VER-52296

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