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Submit ReviewPU H71
Description: Potent Hsp90 inhibitor
Chemical Name: 6-Amino-8-[(6-iodo-1,3-benzodioxol-5-yl)thio]-N-(1-methylethyl)-9H-purine-9-propanamine
Purity: ≥98% (HPLC)
Biological Activity
Potent inhibitor of heat shock protein 90 (Hsp90) (IC50 = 51 nM in MDA-MB-468 cells). Also inhibits cell growth in a range of breast cancer cell lines (IC50 values are 17, 31, 65, 87 and 140 nM for SKBr3, MCF-7, MDA-MB-468, HCC-1806 and MDA-MB-231 cells respectively). Shown to inhibit cell proliferation and induce apoptosis in triple-negative breast cancer (TNBC) cells.
Technical Data
| M. Wt | 512.37 |
| Formula | C18H21IN6O2S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 873436-91-0 |
| PubChem ID | 9549213 |
| InChI Key | SUPVGFZUWFMATN-UHFFFAOYSA-N |
| Smiles | IC1=CC4=C(OCO4)C=C1SC3=NC2=C(N)N=CN=C2N3CCCNC(C)C |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 51.24 | 100 | |
| 1eq. HCl | 51.24 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 512.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.95 mL | 9.76 mL | 19.52 mL |
| 5 mM | 0.39 mL | 1.95 mL | 3.9 mL |
| 10 mM | 0.2 mL | 0.98 mL | 1.95 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
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References
References are publications that support the biological activity of the product.
He et al (2006) Identification of potent water soluble purine-scaffold inhibitors of the heat shock protein 90. J.Med.Chem. 49 381 PMID: 16392823
Chan et al (2008) Molecular imaging of the efficacy of heat shock protein 90 inhibitors in living subjects. Cancer Res. 68 216 PMID: 18172314
Caldas-Lopes et al (2009) Hsp90 inhibitor, PU-H71, a multimodal inhibitor of malignancy, induces complete responses in triple-negative breast cancer models. Proc.Natl.Acad.Sci.USA 106 8368 PMID: 19416831
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Keywords: PU H71, PU H71 supplier, PUH71, heat, shock, proteins, hsp90, inhibitors, inhibits, potent, Hsp90, 3104, Tocris Bioscience
4 Citations for PU H71
Citations are publications that use Tocris products. Selected citations for PU H71 include:
Li et al (2016) PU-H71, a novel Hsp90 inhibitor, as a potential cancer-specific sensitizer to carbon-ion beam therapy. J Radiat Res 57 572 PMID: 27242340
Lee et al (2016) The purine scaffold Hsp90 inhibitor PU-H71 sensitizes cancer cells to heavy ion radiation by inhibiting DNA repair by homologous recombination and non-homologous end joining. Radiother Oncol 121 162 PMID: 27666928
Orozco-Díaz et al (2019) The interaction between RE1-silencing transcription factor (REST) and heat shock protein 90 as new therapeutic target against Huntington's disease. PLoS One 14 e0220393 PMID: 31361762
Echeverría et al (2019) The sensitivity to Hsp90 inhibitors of both normal and oncogenically transformed cells is determined by the equilibrium between cellular quiescence and activity. PLoS One 14 e0208287 PMID: 30726209
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