Catalog No.S8039 Synonyms: NSC 750424

PU-H71 Chemical Structure

Molecular Weight(MW): 512.37

PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.

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  • Effects of low-level HSP90 inhibition (by ganetespib, 2-5 nM; PU-H71, 40-70 nM) or febrile-range temperature (39 ℃) on HSP70 and HSP90 protein levels in FANCA wild-type cells. High-level HSP90 inhibition (ganetespib, 25 nM; PU-H71, 300 nM) as well as proteotoxic proteasomal inhibition (MG132, 2.5 mM) induced the expression of HSP70. Constitutive (upper band: C) and inducible forms (lower band: I) of HSP70 are indicated. HSP90 levels are shown for comparison.

    Cell, 2017, 168(5):856-866. PU-H71 purchased from Selleck.

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Biological Activity

Description PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.
Features Purine-based, HSP90-selective inhibitor.
HSP90 [1]
51 nM
In vitro

PU-H71 (1 μM) potently suppresses the growth of triple-negative breast cancers (TNBC) cell lines MDA-MB-468, MDA-MB-231, and HCC-1806 with IC50 of 65, 140 and 87 nM, respectively. PU-H71 (1 μM) kills 80%, 65%, and 80% of the initial population of MDA-MB-468, MDA-MB-231, and HCC-1806 cells, respectively. PU-H71 (0.25-1 μM) induces a dose-dependent degradation or inactivation of tumor driving molecules, including EGFR, IGF1R, HER3, c-Kit, Raf-1and Akt. Treatment for 24 h with 1 μM PU-H71, augments the percent of cells in G2-M phase of MDA-MB-468 to 69%, mediated by reduction in CDK1 and Chk1 expression. PU-H71 induces apoptosis in TNBC in part by inactivation and downregulation of Akt and Bcl-xL. PU-H71 leads to a proteasome-mediated reduction in IRAK-1 and TBK1 levels, resulting in approximately 84% and 90% reduction in NF-κB activity in MDA-MB-231 cells treated with 0.5 and 1μM PU-H71, respectively. PU-H71 markedly contains MDA-MB-231 cell invasion, with 90% suppression at 1 μM. [1] PU-H71 (2.5 μM) generates endoplasmic reticulum (ER) stress and activated the Unfolded Protein Response (UPR) as evidenced by XBP1 mRNA splicing (2.3-fold) and up-regulation of Grp94 (3.7-fold), Grp78 (4.9-fold), and CHOP (48-fold) protein expression and ATF4 (1.8-fold) mRNA expression. PU-H71 (1 μM) induces the mitochondrial pathway of apoptosis in HeLa cells, mediated by caspase but not calpain activation. In response to PU-H71-induced ER stress, apoptosis is triggered in melanoma, cervix, colon, liver and lung cancer cells, but not in normal human fibroblasts. PU-H71 is able to induce apoptosis overcoming the resistance conferred by Bcl-2. [2] PU-H71 (30 n M) significantly reduces NOS2 activity (60% reduction) and expression in LI (1 μg/mL LPS and 5 ng/mL IFN γ)-stimulated astrocytes via inhibiting NF-κB element activation. PU-H71 displays similar effects on microglial cells as on astrocytes, with 50 nM PU-H71 needed to significantly reduce the LPS dependent nitrite release. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-468 cells MYjGeY5kfGmxbjDhd5NigQ>? NH7kUYNKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUHOyOUCgbY4hcHWvYX6gZpJm[XO2IHPhcoNmeiCPRFGtUWIuPDZ6IHPlcIwhdGmwZTygSWM2OD1yLkCxNFIh|ryP NXGyVGhrOTZ|OUK4NlM>
SKBr3 cells MnvmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWDHdo94fGhiaX7obYJqfGmxbjDpckBpfW2jbjDidoVie3RiY3HuZ4VzKFONQoKzJINmdGxibHnu[UB2e2mwZzDTVmItKEmFNUC9NE4xPSEQvF2= M3jCUlE3Ozl{OEKz
MCF7 cells MlnLSpVv[3Srb36gZZN{[Xl? MkPQNlQhcA>? Mmj1TY5pcWKrdHnvckBw\iCKc4C5NEBqdiCqdX3hckBOS0Z5IHPlcIx{KGG|c3Xzd4VlKGG|IFjldlIhdGW4ZXygZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEwhUUN3ME2wMlA3KM7:TR?= MoXVNVg2PzF7Mkm=
MRC5 cells MnjVR5l1d3SxeHnjbZR6KGG|c3H5 NGXTd4VEgXSxdH;4bYNqfHliYXfhbY5{fCCwb4LtZYwhdHWwZzDmbYJzd2KuYYP0JG1TSzViY3XscEBtcW6nLDDJR|UxRTFizszN MojBNVY{QTJ6MkO=
NCI-H1299 cells NIfOOIJHfW6ldHnvckBie3OjeR?= M3PkNlEzKGh? MV;S[YR2[3Srb36gbY4hd3i7Z3XuJINwdnO3bYD0bY9vKHKjdHWgbY4hcHWvYX6gUmNKNUhzMkm5JINmdGy|IHnuZ5Vj[XSnZDDmc5IhOTJiaILz MVWyOVM5OzlzNR?=
NCI-H69 cells NVPhSoZmTnWwY4Tpc44h[XO|YYm= MV6yOEBp NFPRU5lDcW6maX7nJIFn\mmwaYT5JJRwKEiVUEmwJIlvKGi3bXHuJG5EUS2KNkmgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO|YYm= MnzZNVc3ODN3NEC=
NCI-N417 cells M{jLU2Z2dmO2aX;uJIF{e2G7 M161eVI1KGh? MWnCbY5lcW6pIHHm[olvcXS7IITvJGhUWDlyIHnuJIh2dWGwIF7DTU1PPDF5IHPlcIx{KGGodHXyJFI1KGi{czDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7 NGPpUlEyPzZyM{W0NC=>
NCI-H187 cells M{Tvb2Z2dmO2aX;uJIF{e2G7 Ml7VNlQhcA>? MULCbY5lcW6pIHHm[olvcXS7IITvJGhUWDlyIHnuJIh2dWGwIF7DTU1JOTh5IHPlcIx{KGGodHXyJFI1KGi{czDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7 Ml7ENVc3ODN3NEC=
NCI-H510 cells NYm4PYN{TnWwY4Tpc44h[XO|YYm= MWeyOEBp MW\CbY5lcW6pIHHm[olvcXS7IITvJGhUWDlyIHnuJIh2dWGwIF7DTU1JPTFyIHPlcIx{KGGodHXyJFI1KGi{czDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7 NXLvd4N6OTd4MEO1OFA>
SKBR3 cells Mn7ESpVv[3Srb36gZZN{[Xl? M3;UTlI1KGh? M1nXfWJqdmSrbnegZYZncW6rdImgeI8hUFOSOUCgbY4hcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JIZtfW:{ZYPj[Y5k\SCyb3zhdol7[XSrb36gZZN{[Xl? NHLiSpAyPzZyM{W0NC=>
NCI-H526 cells NEDFcnlHfW6ldHnvckBie3OjeR?= MWmxJO69VQ>? MUeyOEBp NX;LfJpbSmmwZHnu[{Bi\m[rbnn0fUB1dyCKU2C5NEBqdiCqdX3hckBPS0lvSEWyOkBk\WyuczDheEAyKHWPIHHmeIVzKDJ2IHjyd{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG|c3H5 NYi3UphkOTd4MEO1OFA>
H69AR cells NGX0Xm9HfW6ldHnvckBie3OjeR?= M1PSRlk3KGh? MV3Jcohq[mm2aX;uJI9nKEiVUEmwMY1m\GmjdHXkJIFvfGmjcH;weI91cWNiYXP0bZZqfHliaX6gbJVu[W5iSE[5RXIh[2WubIOgZZN{\XO|ZXSgZZMhcW6mdXP0bY9vKG:oIHPlcIwh\3Kxd4ToJIFzemW|dDDheEAyOCCjZoTldkA6PiCqcoOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcI94KGO7dH;t[ZRzgQ>? Mkf6NVc3ODN3NEC=
NCI-H526 cells MX;GeY5kfGmxbjDhd5NigQ>? NUfJ[YlsOjRiaB?= MV7CbY5lcW6pIHHm[olvcXS7IITvJGhUWDlyIHnuJIh2dWGwIF7DTU1JPTJ4IHPlcIx{KGGodHXyJFI1KGi{czDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7 MUmxO|YxOzV2MB?=

... Click to View More Cell Line Experimental Data

In vivo PU-H71 administered at 75 mg/kg a.d. in the MDA-MB-231 model, induces a 100% complete response, and tumors are reduced to scar tissue after 37 days of treatment, accompanied with reduction in many proliferative and anti-apoptotic molecules, namely an 80%, 95%, 99%, 80%, and 65% decrease in EGFR, HER3, Raf-1, Akt, and p-Akt, respectively. PU-H71 (75 mg/kg, 3 times per week) induces a 96% inhibition of tumor growth, accompanied by an 60% reduction in tumor cell proliferation, an 85% decline in activated Akt associated with survival and high invasive potential, and a 6-fold increase in apoptosis. [1]


Kinase Assay:


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HSP90 binding assay:

Measurements are performed in black 96-well microtiter plates. Cell lysates are prepared by rupturing cellular membranes by freezing at -70℃ and dissolving the cellular extract in HFB [20 mM Hepes (K), pH 7.3, 50 mM KCl, 5 mM MgCl2, 20 mM Na2MoO4, 0.01% Nonidet P-40] with added protease and phosphatase inhibitors. Saturation curves are recorded in which fluorescently labeled geldanamycin (Cy3B-GM) (3 nM) is treated with increasing amounts of cellular lysates. The amount of lysate that results in polarization (mP) readings corresponding to 90%-99% bound ligand is chosen for the competition study. Here, each 96-well plate contains 3 nM Cy3B-GM, cellular lysate (amounts as determined and normalized to total Hsp90 as determined by Western blot analysis using Hsp90 purified from HeLa cells as standard) and tested Hsp90 inhibitor in a final volume of 100 μL. The plate is left for 24 h on a shaker at 4 ℃, and the fluorescence polarization (FP) values in mP are recorded. EC50 values are determined as the competitor concentrations at which 50% of the Cy3B-GM is displaced. FP measurements are performed on an Analyst GT microplate reader.
Cell Research:


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  • Cell lines: Human triple-negative breast cancers cell line MDA-MB-231
  • Concentrations: ~5μM
  • Incubation Time: 3 days
  • Method:

    Exponentially growing MDA-MB-231 cells are seeded into black 96-well microtiter plates and incubated in medium containing either vehicle control (DMSO) or compounds for the indicated time at 37 ℃. Plates containing 3 replicate wells per assay condition are seeded at a density of 8×103 cells for each cell line in 100μL medium. After exposure of cells to the Hsp90 inhibitors, plates are equilibrated to room temperature (20-25 ℃) for approximately 30 min, and 100 μL CellTiter-Glo reagent are added to each well. Plates are mixed for 2 min on an orbital shaker and then incubated for 15 min to 2 h at room temperature. The luminescence signal in each well is measured in an Analyst GT microplate reader.

    (Only for Reference)
Animal Research:


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  • Animal Models: Human triple-negative breast cancers xenografts MDA-MB-231
  • Formulation: PBS
  • Dosages: 75 mg/kg
  • Administration: i.p. on an alternate day schedule
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (195.17 mM)
Ethanol 100 mg/mL (195.17 mM)
Water 34 mg/mL warmed (66.35 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 512.37

C18 H21 I N6 O2 S

CAS No. 873436-91-0
Storage powder
in solvent
Synonyms NSC 750424

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01581541 Terminated Solid Tumors|Lymphoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) April 26 2011 Phase 1
NCT03373877 Recruiting Myelofibrosis|Primary Myelofibrosis|Post-polycythemia Vera Myelofibrosis|Post-essential Thrombocythemia Myelofibrosis Samus Therapeutics Inc. May 24 2018 Phase 1
NCT03166085 Recruiting Metastatic Breast Cancer Memorial Sloan Kettering Cancer Center|Samus Therapeutics Inc. May 23 2017 Phase 1
NCT01393509 Active not recruiting Metastatic Solid Tumor|Lymphoma|Myeloproliferative Neoplasms (MPN) Memorial Sloan Kettering Cancer Center July 2011 Phase 1
NCT01269593 Recruiting Non-Hodgkin''s Lymphoma|Myeloma|Active Solid Malignancy Memorial Sloan Kettering Cancer Center|Samus Therapeutics December 2010 Early Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID