Geldanamycin

Catalog No.S2713 Synonyms: NSC 122750

Geldanamycin Chemical Structure

Molecular Weight(MW): 560.64

Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.

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3 Customer Reviews

  • Phenotypic effect of Genetic or Pharmacologic Compromise of the 477 Hsp70-StiA-Hsp90 Complex. The impact of each genetic modification on radial growth, conidiation, and response to various stress conditions was assessed after inoculation of a suspension of 104 conidia on glucose minimal medium (GMM) agar plates and incubation at 37ºC for 5 days.

    Antimicrob Agents Chemother, 2015, 10.1128/AAC.00946-15. Geldanamycin purchased from Selleck.

    C2C12 myoblasts were transfected with HA-tagged A17-PABPN1 constructs. Twenty-four hours post-transfection, cells were treated with CHX (10 μg/ml) alone or together with geldanamycin (2.5 μM) for the indicated times at 37°C. Lysates were blotted to show the expression of the proteins of interest. Band density was quantified and is shown in the line graph (right panels). Data are shown as the mean ± SEM (n = 5); **, P < 0.01.

    PLoS One, 2015, 10(9):e0138936.. Geldanamycin purchased from Selleck.

  • RT-qPCR analysis of eNOS mRNA and representative Western blot images of eNOS expression, respectively, in irradiated BAECs pretreated of geldanamycin (GA; 500 nM). At 12 h after 10 Gy irradiation, BAECs were harvested. The results suggest that both HSP90 is involved in the upregulation of eNOS in irradiated BAECs.

    Radiat Res, 2018, 189(5):519-528. Geldanamycin purchased from Selleck.

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Choose Selective HSP (e.g. HSP90) Inhibitors

Biological Activity

Description Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.
Targets
p185 [4]
(SKBr3 cells)
HSP90 (N-terminal domain) [1]
(Cell-free assay)
HSP90 [1]
(Cell-free assay)
70 nM 0.78 μM(Kd) 1.2 μM(Kd)
In vitro

Geldanamycin binds in the ATP-binding site in the N-terminus domain of Hsp90s (residues 1-220). Geldanamycin inhibits the ATPase activity of Hsp90 in a dose-dependent manner. [1] Geldanamycin causes a dose-dependent G2 arrest and reversible inhibiton o f entry into the S phase in A2780 human ovarian cell line. This inhibition is accompanied by p53 increase and finally demonstrated to be p53 dependent. [2] Geldanamycin causes polyubiquitination and proteasomal degradation of the p185 receptor protein-tyrosin kinase and shows a IC50 with 70 nM. [3, 4] Geldanamycin is a typical anti-tumor reagent, shows a mean GI50 with 0.18 μM against the panel of 60 human tumor cell lines. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A2780 cells MorKVJJwdGmoZYLheIlwdiCjc4PhfS=> NEDORYxEd22yb4Xu[EB4[XNiZY\hcJVifGWmIH\vdkBidnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIH;2ZZJq[W5iY3HyZ4lvd22jIHPlcIwhdGmwZTDBNlc5OCxiSVO1NF0{NjRizszN M{LuTVEyPTF2MUS1
SW620 cell M2e4PGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmXPTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiaIXtZY4h[2:ub4LlZ5RidCClYYLjbY5wdWFiU2e2NlAh[2WubDDsbY5meyxiSVO1NF03NjJibl2= NGPkZ40yPTZ3OEi3PS=>
MCF-7 cell NWjaPHFlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXrJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCqdX3hckBjemWjc4SgZ4Fv[2W{IF3DSk04KGOnbHygcIlv\XNuIFnDOVA:Pi53IH7N NV\1[3ZJOTV4NUi4O|k>
SKBR3 cells NITafXNRem:uaX\ldoF1cW:wIHHzd4F6 MXW3NkBp MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHXzeJJw\2WwIILlZ4VxfG:{IHTl[olkcWWwdDDoeY1idiCVS1LSN{Bk\WyuczDh[pRmeiB5MjDodpMtKEmFNUC9PE42KG6P M3XsRlI{PjR6MUiw
MCF7 cells M33hS3Bzd2yrZnXyZZRqd25iYYPzZZk> NFj1SFE4OiCq MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiZYjwdoV{e2mwZzDld5Rzd2enbjDy[YNmeHSxcjDh[pRmeiB5MjDodpMtKEmFNUC9PU45KG6P NXLQSWFGOjN4NEixPFA>
MDA-kb2 cells M174bmZ2dmO2aX;uJIF{e2G7 MmLtNVghcA>? NXvYNHdMUW6qaXLpeIlwdiCxZjDIV3A6OCCrbjDoeY1idiCPRFGtb4IzKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDncJVkd2OxcoTpZ49q\CC{ZXPldJRwei2mZYDlcoRmdnRibIXjbYZmemG|ZTDlfJBz\XO|aX;uJIFnfGW{IEG4JIhzeyCkeTDmbZJm\my7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhUUN3ME2xNEBvVQ>? NHu5R3QzPDl6NEmzOi=>
human SK-BR-3 cells NHHq[2JRem:uaX\ldoF1cW:wIHHzd4F6 MVXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLVLSMVMh[2WubIOsJGlEPTB;MUWuPEBvVQ>? MUixPVg6Pjh2OB?=
HUVEC cells M1j1ZmN6fG:2b4jpZ:Kh[XO|YYm= Mm\3O|IhcA>? MVvDfZRwfG:6aXPpeJkh[WejaX7zeEBJXV[HQzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVE6KG6P NWLqdnRUOjV{N{ewOlc>
human HCT116 cells Mn74S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MofxS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTGNVOTF4IHPlcIx{NCCJSUWwQVIyKG6P NVrFWm9FOTh{NEO3NFM>
K562 cell MlHFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3TPfmlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IHj1cYFvKGyndXvlcYliKEt3NkKgZ4VtdCCuaX7ld{whUUN3ME2yNk4yKG6P NETvUmIyPTZ3OEi3PS=>
HT-29 cell NEXzfFdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGWyUoRKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDoeY1idiClb3zvdoVkfGGuIHPhdoNqdm:vYTDIWE0zQSClZXzsJIxqdmW|LDDJR|UxRTJ2LkWgcm0> M{ntNVE2PjV6OEe5
HCT116 cells MYLQdo9tcW[ncnH0bY9vKGG|c3H5 NESxelBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BjgSCudX3pcoV{[2WwY3WgZZN{[XluIFXDOVA:OC5yMzFOwG0> MXuyNVYxPTl5NR?=
NCI-H1975 cells M{LuU3Bzd2yrZnXyZZRqd25iYYPzZZk> M{DOXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgyQTd3IHPlcIx{NCCLQ{WwQVM3KG6P M1LYXlIyPzF3MU[1
human DLD1 cells MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4jEfWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGRNTDFiY3XscJMtKEeLNUC9N|chdk1? M4[yfFE5OjR|N{Cz
human A431 cells NGXpXnhEgXSxdH;4bYPDqGG|c3H5 MUG3NkBp NGjMPHZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OFAhdk1? NH3zfY0zPTJ5N{C2Oy=>
human HepG2 cells NUT3bodjS3m2b4TvfIlkyqCjc4PhfS=> MUO3NkBp NWTnXWZMS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF01OCCwTR?= MYOyOVI4PzB4Nx?=
human BGC823 cells NV7lWIJ2S3m2b4TvfIlkyqCjc4PhfS=> NVX6fXJNPzJiaB?= M{PKO2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJISzh{MzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVQxKG6P NF;QbmQzPTJ5N{C2Oy=>
human SKBR3 cells MlLOR5l1d3SxeHnjxsBie3OjeR?= M2XRSlczKGh? M4XBVWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMSlJ|IHPlcIx{KGGodHXyJFczKGi{czDifUBk\WyudHn0[ZIu\2yxIHHzd4F6NCCLQ{WwQVQyKG6P NXTTc|J{OTl2MEW1Nlg>
human MDA-MB-231 cells Ml[wR5l1d3SxeHnjxsBie3OjeR?= MWe3NkBp NIj5eGVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NUCgcm0> NIOz[oMzPTJ5N{C2Oy=>
human A549 cells MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{nGUGdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGE2PDliY3XscJMtKEeLNUC9OlQhdk1? NX3lTlhVOTh{NEO3NFM>
Sf9 cells NEHaUZpHfW6ldHnvckBie3OjeR?= NHzXfGdFcXOybHHj[Y1mdnRib3[gS20uSk:GSWDZJIZzd21iaIXtZY4h\nWubDDs[Y5ofGhiSGPQPVAh[WyyaHGg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|LXnu[oVkfGWmIGPmPUBk\WyuczDh[pRmeiBzNjDodpMh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhUUN3ME23OEBvVQ>? MYmyOFc2OTR2MR?=
human U87MG cells NYXpUlBUWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml6yRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXOEfNS{Bk\WyuczygTWM2OD16OTDuUS=> NIrCU4MzOTdzNUG2OS=>
human A549 cells NWPlOYJuS3m2b4TvfIlkyqCjc4PhfS=> Mn3TO|IhcA>? MlPWR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUm3JI5O NVjuclU5OjV{N{ewOlc>
mouse P19 cells M2nkW2N6fG:2b4jpZ:Kh[XO|YYm= Mnz1NVghcA>? NXHqRWZCS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhWDF7IHPlcIx{KGGodHXyJFE5KGi{czygTWM2OD1yLkGg{txO NVjCZZluOTd2NEK1OlU>
human HL7702 cells NFrXR|hEgXSxdH;4bYPDqGG|c3H5 NGr0bpA4OiCq NFnSc3VEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVDd5MEKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjF2MTFOwG0> NHzZeo0zPTJ5N{C2Oy=>
human A549 cells MnXhR5l1d3SxeHnjxsBie3OjeR?= M1rLN|Ih\GG7cx?= M3PQSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgNkBl[Xm|IHL5JGFt[W2jclLseYUh[XO|YYmsJGlEPTB;MD6xOUDPxE1? M{\mTlI{QTR5N{m0
human A431 cells M3\OfXBzd2yrZnXyZZRqd25iYYPzZZk> MXG3NkBp NGTH[WVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0N|Eh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVAvOiEQvF2= M1rpe|IxPjV3MkO3
human HepG2 cells M4jobWN6fG:2b4jpZ:Kh[XO|YYm= M4XzZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1yLkOg{txO M4XVcFI{PjV4NUW2
human SW480 cells NYDOcphES3m2b4TvfIlkyqCjc4PhfS=> NF;IZWM4OiCq NEHPbm1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUXzR6MDDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOzFizszN Mn;JNlUzPzdyNke=
human LNCAP cells NXHj[Ws4S3m2b4TvfIlkyqCjc4PhfS=> NHH6RWI4OiCq NUnBNotCS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVE6FQWCgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjR|IN88US=> NVfZTpNlOjVzMEW5NlQ>
human LS174T cells NHu1cnBEgXSxdH;4bYPDqGG|c3H5 MX7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMV|E4PFRiY3XscJMh[nliTWTTJIF{e2G7LDDJR|UxRTBwNEWg{txO NFrwTlEyPzB|NEGzOS=>
human HeLa cells M{HqWWN6fG:2b4jpZ:Kh[XO|YYm= NFjhR4Q4OiCq M{HCZWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmVGFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlc6QCEQvF2= MkTMNlUzPzdyNke=
rat L6 cells NVjrU4x1S3m2b4TvfIlkyqCjc4PhfS=> MWG3NkBp NV35UolsS3m2b4TvfIlkcXS7IHHnZYlve3RicnH0JGw3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDBcIFu[XJiQnz1[UBie3OjeTygTWM2OD13IN88US=> M2fVZ|I1PThyNUOx
human MCF7 cells NGXK[5JEgXSxdH;4bYPDqGG|c3H5 MV3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIJ6KFOUQjDhd5NigSxiSVO1NF06NjZizszN NHnqXosyQTV4MEO1Ny=>
human MCF7 cells NIXaTY5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIK0[WFIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJIRigXNiYomgV3JDKGG|c3H5MEBIUTVyPUO1MlYh|ryP MV6xO|g3QTB7OB?=
HEK293T cells NXjtZ4NTTnWwY4Tpc44h[XO|YYm= NYrPcZVTUW6qaXLpeIlwdiCxZjDUUmYu[WyyaHGtbY5lfWOnZDDOSk1s[XCyYVKgZYN1cX[jdHnvckBmgHC{ZYPz[YQhcW5iSFXLNlk{XCClZXzsd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= M4HPO|E5PDB6N{Gz
human Jurkat cells MnmwSpVv[3Srb36gZZN{[Xl? MWLJcohq[mm2aX;uJI9nKFSQRj3hcJBp[S2rbnT1Z4VlKE6ILXvhdJBiSiCjY4TpeoF1cW:wIHX4dJJme3OnZDDpckBHSUSGIHTl[olkcWWwdDDoeY1idiCMdYLrZZQh[2WubIOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7 NYPmeJZ7OTh2MEi3NVM>
human SKBR3 cells NInFTlJHfW6ldHnvckBie3OjeR?= NWPiZ4lGOjRiaB?= NH\5XoZKdmirYnn0bY9vKG:oIFjzdFkxNW2nZHnheIVlKEiHUkKg[IVoemGmYYTpc44hcW5iaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdB?= M{PQd|E5QDF4MUGx

... Click to View More Cell Line Experimental Data

In vivo Geldanamycin (50 mg//kg) shows 30% inhibition on pl85-associated phosphotyrosine levels in FRE/erbB-2 mice. [6]

Protocol

Kinase Assay:

[1]

+ Expand

Isothermal Titration Calorimetry (ITC) of Nucelotide Binding:

The titration experiments are performed using the MSC system. In each experiment, 16 aliquots of 15 μL of geldanamycin (300 μM in 1% DMSO) are injected into 1.3 mL of protein (31 μM in 20 mMTris-HCl, pH 7.5, 1 mMEDTA) at 25 °C, and the resulting data are fit after subtracting the heats of dilution. Heats of dilution are determined in separate experiments from addition of geldanamycin into buffer and buffer into protein. No evidence for binding of DMSO in the nucleotide binding site is observed. Titration data are fit using a nonlinear least-squares curve-fitting algorithm with three floating variables: stoichiometry, binding constant (Kb) 1/Kd), and change of enthalpy of interaction (ΔH°). Dissociation constants estimated for geldanamycin binding to intact yeast Hsp90 is 1.22 μM, and for binding to Hsp90 N-terminal domain is 0.78 μM. No meaningful heat is observed with binding to the C-terminal fragment.
Cell Research:

[2]

+ Expand
  • Cell lines: A2780 human ovarian cell line
  • Concentrations: 0.001-10 μM
  • Incubation Time: 3 hours
  • Method:

    Exponentially growing cells are treated with Geldanamycin and at various times DNA synthesis is assessed by incorporation of bromodeoxyuridine (BrdUrd) and flow cytometric analysis. No marked difference in total cell number is noted during this time course for treated and untreated cultures. BrdUrd (10 μM) is incorporated over a 4-h incubation period at 37 °C and cells are harvested and fixed in 70% ethanol. After denaturation of the DNA with 2 N HC1, cells are incubated with an anti-BrdUrd mouse monoclonal antibody followed by a fluorescein isothiocyanate (FITC)-linked goat anti-mouse IgG. Cells are stained for 30 minutes at room temperature with propidium iodide and analysed by flow cytometry using a Coulter EPICS Profile Analyzer.


    (Only for Reference)
Animal Research:

[6]

+ Expand
  • Animal Models: FRE/erbB-2 tumors in nu/nu mice
  • Formulation: Geldanamycin is dissolved in DMSO.
  • Dosages: 50 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 36 mg/mL warmed (64.21 mM)
Water Insoluble
Ethanol Insoluble

* 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 560.64
Formula

C29H40N2O9

CAS No. 30562-34-6
Storage powder
in solvent
Synonyms NSC 122750

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID