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Geldanamycin

Catalog No. T6343 CAS 30562-34-6

Synonyms: 格尔德霉素, NSC 122750

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

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Geldanamycin, CAS 30562-34-6

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Purity: 98%

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Chemical Properties

Storage & Solubility Information

Description	Geldanamycin, an HSP90 inhibitor (Kd: 1.2 μM), specifically disrupts glucocorticoid receptor (GR)/HSP association.
Targets&IC50	p185:70 nM, HSP90:1.2 μM(Kd), HSP90 (N-terminal domain):0.78 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]
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	格尔德霉素, NSC 122750
Molecular Weight	560.644
Formula	C29H40N2O9
CAS No.	30562-34-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

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

H2O: <1 mg/mL

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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.

Citations

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：

Anti-Cancer Compound Library Endoplasmic Reticulum Stress Compound Library Preclinical Compound Library Autophagy Compound Library HIF-1 Signaling Pathway Compound Library Inhibitor Library Macrocyclic Compound Library Natural Product Library for HTS Anti-Tumor Natural Product Library Oxidation-Reduction Compound Library

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Keywords

Geldanamycin 30562-34-6 代谢蛋白酪氨酸激酶微生物学细胞骨架 Antibacterial Antibiotic HSP Influenza Virus Tyrosine Kinases Bacterial inhibit Inhibitor NSC 122750 Heat shock proteins inhibitor

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