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 M2nBPGZ2dmO2aX;uJIF{e2G7 MX7Jcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgTJNxQTBiaX6gbJVu[W5iYoLlZZN1KGOjbnPldkBOTEFvTVKtOFY5KGOnbHygcIlv\SxiRVO1NF0xNjBzMEKg{txO M3zFOVE3Ozl{OEKz
SKBr3 cells MmXtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH7pU4VIem:5dHigbY5pcWKrdHnvckBqdiCqdX3hckBjemWjc4SgZ4Fv[2W{IGPLRpI{KGOnbHygcIlv\SC3c3nu[{BUWkJuIFnDOVA:OC5yNTFOwG0> MUmxOlM6Ojh{Mx?=
MCF7 cells NVfQSGZSTnWwY4Tpc44h[XO|YYm= NEPCclEzPCCq M1e5UWlvcGmkaYTpc44hd2ZiSIPwPVAhcW5iaIXtZY4hVUOINzDj[YxteyCjc4Pld5Nm\CCjczDI[ZIzKGyndnXsJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5QtKEmFNUC9NE4xPiEQvF2= M2XBSFE5PTdzOUK5
MRC5 cells Mn\SR5l1d3SxeHnjbZR6KGG|c3H5 M13h[2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KG6xcn3hcEBtfW6pIH\pZpJw[myjc4SgUXJEPSClZXzsJIxqdmVuIFnDOVA:OSEQvF2= MX:xOlM6Ojh{Mx?=
NCI-H1299 cells NWXuVmhVTnWwY4Tpc44h[XO|YYm= NGHxWJkyOiCq NUXIO4xwWmWmdXP0bY9vKGmwIH;4fYdmdiClb37zeY1xfGmxbjDyZZRmKGmwIHj1cYFvKE6FST3INVI6QSClZXzsd{BqdmO3YnH0[YQh\m:{IEGyJIhzew>? M3fzdFI2Ozh|OUG1
NCI-H69 cells MlTwSpVv[3Srb36gZZN{[Xl? NITjc|QzPCCq NYTXVW9wSmmwZHnu[{Bi\m[rbnn0fUB1dyCKU2C5NEBqdiCqdX3hckBPS0lvSE[5JINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG|c3H5 NHzmOFIyPzZyM{W0NC=>
NCI-N417 cells M1fqZ2Z2dmO2aX;uJIF{e2G7 NX:zUGRqOjRiaB?= MY\CbY5lcW6pIHHm[olvcXS7IITvJGhUWDlyIHnuJIh2dWGwIF7DTU1PPDF5IHPlcIx{KGGodHXyJFI1KGi{czDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7 Ml;5NVc3ODN3NEC=
NCI-H187 cells NUXDcIMyTnWwY4Tpc44h[XO|YYm= MmLSNlQhcA>? NEnsOGtDcW6maX7nJIFn\mmwaYT5JJRwKEiVUEmwJIlvKGi3bXHuJG5EUS2KMUi3JINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG|c3H5 NE\X[IIyPzZyM{W0NC=>
NCI-H510 cells NFrt[mNHfW6ldHnvckBie3OjeR?= NEXZUIEzPCCq NXzoNZYySmmwZHnu[{Bi\m[rbnn0fUB1dyCKU2C5NEBqdiCqdX3hckBPS0lvSEWxNEBk\WyuczDh[pRmeiB{NDDodpMh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfS=> NVXBUmxkOTd4MEO1OFA>
SKBR3 cells NF\F[IdHfW6ldHnvckBie3OjeR?= M3LvOVI1KGh? M3vTRWJqdmSrbnegZYZncW6rdImgeI8hUFOSOUCgbY4hcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JIZtfW:{ZYPj[Y5k\SCyb3zhdol7[XSrb36gZZN{[Xl? NV73UWJROTd4MEO1OFA>
NCI-H526 cells MmXiSpVv[3Srb36gZZN{[Xl? NHfvbJkyKM7:TR?= MkXtNlQhcA>? Ml33Rolv\GmwZzDh[oZqdmm2eTD0c{BJW1B7MDDpckBpfW2jbjDOR2kuUDV{NjDj[YxteyCjdDCxJJVOKGGodHXyJFI1KGi{czDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7 NIr4RZoyPzZyM{W0NC=>
H69AR cells MoLLSpVv[3Srb36gZZN{[Xl? M1O2U|k3KGh? NYDnbHdpUW6qaXLpeIlwdiCxZjDIV3A6OC2vZXTpZZRm\CCjboTpZZBweHSxdHnjJIFkfGm4aYT5JIlvKGi3bXHuJGg3QUGUIHPlcIx{KGG|c3Xzd4VlKGG|IHnu[JVkfGmxbjDv[kBk\WyuIHfyc5d1cCCjcoLld5Qh[XRiMUCgZYZ1\XJiOU[gbJJ{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\myxdzDjfZRwdWW2com= MkXjNVc3ODN3NEC=
NCI-H526 cells MYDGeY5kfGmxbjDhd5NigQ>? MnfGNlQhcA>? NUnsN4RVSmmwZHnu[{Bi\m[rbnn0fUB1dyCKU2C5NEBqdiCqdX3hckBPS0lvSEWyOkBk\WyuczDh[pRmeiB{NDDodpMh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfS=> M3Oz[FE4PjB|NUSw

... 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
Synonyms NSC 750424

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01581541 Completed Solid Tumors|Lymphoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) April 26, 2011 Phase 1
NCT01393509 Recruiting Metastatic Solid Tumor|Lymphoma|Myeloproliferative Neoplasms (MPN) Memorial Sloan Kettering Cancer Center July 2011 Phase 1
NCT01269593 Recruiting Non-Hodgkins 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