Geldanamycin
For research use only. Not for use in humans.
Catalog No.S2713 Synonyms: NSC 122750
12 publications
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.
3 Customer Reviews
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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.
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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. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| In vivo | Geldanamycin (50 mg//kg) shows 30% inhibition on pl85-associated phosphotyrosine levels in FRE/erbB-2 mice. [6] |
Protocol
| Kinase Assay: |
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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. |
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Solubility (25°C)
| In vitro | DMSO | 36 mg/mL warmed (64.21 mM) |
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| 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 |
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| Formula | C29H40N2O9 |
| CAS No. | 30562-34-6 |
| Storage | powder |
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| Synonyms | NSC 122750 |
| Smiles | COC1CC(C)CC2=C(OC)C(=O)C=C(NC(=O)\C(=C\C=C\C(OC)C(OC(N)=O)\C(=C\C(C)C1O)C)C)C2=O |
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