PU H71

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Cat.No. 3104 - PU H71 | C18H21IN6O2S | CAS No. 873436-91-0
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)
Datasheet
Citations (4)
Reviews
Literature (3)

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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets

Certificate of Analysis / Product Datasheet
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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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Literature in this Area

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