PU-H71

SKU: orb1819131

Description

PU-H71 is a potent and selective HSP90 inhibitor, demonstrating an IC50 value of 51 nM. It is widely used in cancer research to study oncogenic client protein degradation in both cellular and animal models of various malignancies.

Research Area

Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 873436-91-0
• MW: 512.37
• Purity: 99.94% (May vary between batches)
• Formula: C₁₈H₂₁IN₆O₂S
• SMILES: CC(C)NCCCn1c(Sc2cc3OCOc3cc2I)nc2c(N)ncnc12
• Target: HSP
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.9 mM);DMSO:46.1 mg/mL (89.97 mM)

Bioactivity

• Target IC50:
  HSP90:51 nM
• In Vivo:
  MDA-MB-231 model treated with PU-H71 at a dose of 75 mg/kg was 100% fully effective. After 37 days of treatment, tumor was replaced by scar tissue, accompanied by a reduction in many proliferative and anti apoptotic molecules, such as EGFR, HER3, Raf-1, Akt, and p-Akt, which decreased by 80%, 95%, 99%, 80%, and 65%, respectively. PU-H71 (75 mg/kg, three times a week) inhibits tumor growth by 96%, reduces tumor cell proliferation by 60%, decreases activated Akt associated with survival and high invasive potential by 85%, and increases apoptosis by 6-fold.
• In Vitro:
  PU-H71(1 μ M) potently inhibits the growth of triple negative breast cancer (TNBC) cell lines MDA-MB-468, MDA-MB-231, and HCC-1806, with IC50 values of 65, 140, and 87 nM, respectively. PU-H71(1 μ M) kills 80%, 65%, and 80% of MDA-MB-468, MDA-MB-231, and HCC-1806 cells, respectively.

Storage & Handling

• Storage: store at low temperature,store under nitrogen | 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

HSP90, PU H71, PUH71, PU-H71

Compound Identifiers

PubChem CID

9549213

Romy Cools # 1, Valeria Narykina # 1 2 3, Koen Vermeulen 4, Sanket J Mishra 5, Brian S J Blagg 5 6, Marleen Derweduwe 7 8 9, Frederik De Smet 7 8 9, Aaron Ziani-Zeryouh 10, Matteo Riva 10 11, An Coosemans 10, Frederic Rousseau 2 3, Joost Schymkowitz 2 3, Guy Bormans 12 [11C]HSP990 PET as a translational tool to investigate the role of Hsp90 in tumours and support the development of Hsp90 therapeutics EJNMMI Radiopharm Chem, (2025)

PubMed: 41003947