Home Tools
Log in
Cart

Geldanamycin

Catalog No. T6343   CAS 30562-34-6
Synonyms: NSC 122750

Geldanamycin, an HSP90 inhibitor (Kd: 1.2 μM), specifically disrupts glucocorticoid receptor (GR)/HSP association.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Geldanamycin Chemical Structure
Geldanamycin, CAS 30562-34-6
Pack Size Availability Price/USD Quantity
10 mg In stock $ 39.00
25 mg In stock $ 72.00
50 mg In stock $ 122.00
100 mg In stock $ 198.00
1 mL * 10 mM (in DMSO) In stock $ 43.00
Bulk Inquiry
Get quote
Select Batch  
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description Geldanamycin, an HSP90 inhibitor (Kd: 1.2 μM), specifically disrupts glucocorticoid receptor (GR)/HSP association.
Targets&IC50 HSP90 (N-terminal domain):0.78 μM(Kd), HSP90:1.2 μM(Kd), p185:70 nM
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]
In vivo Geldanamycin (50 mg//kg) shows 30% inhibition on pl85-associated phosphotyrosine levels in FRE/erbB-2 mice. [6]
Kinase Assay 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 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)
Synonyms NSC 122750
Molecular Weight 560.64
Formula C29H40N2O9
CAS No. 30562-34-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (89.18 mM), warmed

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Roe SM, et al, J Med Chem, 1999, 42(2), 260-266. 2. Mcllwrath AJ, et al, Cancer Chemother Pharmacol, 1996, 37(5), 423-428. 3. Mimnaugh EG, et al, J Biol Chem 1996, 271(37), 22796-22801. 4. Miller P, et al, Cancer Res, 1994, 54(10), 2724-2730. 5. Supko JG, et al, Cancer Chemother Pharmacol, 1995, 36(4), 305-315. 6. Lin Z, et al. 17-ABAG, a novel Geldanamycin derivative, inhibits LNCaP-cell proliferation through heat shock protein 90 inhibition. Int J Mol Med. 2015 Aug;36(2):424-32. 7. Tang HB, et al. Viperin inhibits rabies virus replication via reduced cholesterol and sphingomyelin and is regulated upstream by TLR4. Sci Rep. 2016 Jul 26;6:30529 8. Siddiqui F A, Parkkola H, Vukic V, et al. Novel Small Molecule Hsp90/Cdc37 Interface Inhibitors Indirectly Target K-Ras-Signaling[J]. Cancers. 2021, 13(4): 927. 9. Díaz-Díaz A, Roca-Lema D, Casas-Pais A, et al. Heat Shock Protein 90 Chaperone Regulates the E3 Ubiquitin-Ligase Hakai Protein Stability[J]. Cancers. 2020, 12(1): 215. 10. Wu Z, Geng Y, Lu X, et al. Chaperone-mediated autophagy is involved in the execution of ferroptosis[J]. Proceedings of the National Academy of Sciences. 2019 Feb 19;116(8):2996-3005.

TargetMolCitations

1. Siddiqui F A, Parkkola H, Manoharan G B, et al. Medium-Throughput Detection of Hsp90/Cdc37 Protein-Protein Interaction Inhibitors Using a Split Renilla Luciferase-Based Assay. SLAS DISCOVERY: Advancing the Science of Drug Discovery. 2020, 25(2): 195-206 2. Wu Z, Geng Y, Lu X, et al. Chaperone-mediated autophagy is involved in the execution of ferroptosis. Proceedings of the National Academy of Sciences. 2019 Feb 19;116(8):2996-3005 3. Díaz-Díaz A, Roca-Lema D, Casas-Pais A, et al. Heat Shock Protein 90 Chaperone Regulates the E3 Ubiquitin-Ligase Hakai Protein Stability. Cancers. 2020, 12(1): 215 4. Siddiqui F A, Parkkola H, Vukic V, et al. Novel Small Molecule Hsp90/Cdc37 Interface Inhibitors Indirectly Target K-Ras-Signaling. Cancers. 2021 Feb 23;13(4):927. doi: 10.3390/cancers13040927. 5. Wei Shi, Guang Xu, Xiaoyan Zhan, Yuan Gao, Zhilei Wang, Shubin Fu, Nan Qin, Xiaorong Hou, Yongqiang Ai, Chunyu Wang, Tingting He, Hongbin Liu, Yuanyuan Chen, Yan Liu, Jiabo Wang, Ming Niu, Yuming Guo, Xiaohe Xiao & Zhaofang Bai Carnosol inhibits inflammasome activation by directly targeting HSP90 to treat inflammasome-mediated diseases. Cell Death & Disease. 2020 6. Siddiqui F A, Parkkola H, Manoharan G, et al. Medium-Throughput Detection of Hsp90/Cdc37 Protein–Protein Interaction Inhibitors Using a Split Renilla Luciferase-Based Assay. SLAS Discovery. 2020, 25(2): 195-206

Related compound libraries

This product is contained In the following compound libraries:
Microbial Natural Product Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Preclinical Compound Library Anti-Breast Cancer Compound Library Metabolism Compound Library Anti-Cancer Compound Library Antibiotics Library Cytoskeletal Signaling Pathway Compound Library Macrocyclic Compound Library

Related Products

Related compounds with same targets
SU 4981 Ruxolitinib AMG 900 Ilginatinib hydrochloride NVP-AEW541 Ruxolitinib (S enantiomer) RO495 Gefitinib

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Geldanamycin 30562-34-6 Cytoskeletal Signaling Metabolism Microbiology/Virology Tyrosine Kinase/Adaptors HSP Tyrosine Kinases Influenza Virus Antibiotic Antibacterial NSC-122750 Bacterial NSC122750 inhibit Inhibitor NSC 122750 Heat shock proteins inhibitor

 

TargetMol