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Geldanamycin [30562-34-6]

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Referencia HY-15230-10mg

embalaje : 10mg

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Teléfono : +1 850 650 7790

Marca : MedChemExpress

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Descripciòn

Geldanamycin is a Hsp90 inhibitor with antimicrobial activity against many Gram-positive and some Gram-negative bacteria. Geldanamycin has anti-influenza virus H5N1 activities.

IC₅₀ & Target^[4]

HSP90

1.2 μM (Kd)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.07 μM Compound: 1	Antiproliferative activity against human A2780 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human A2780 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27476419]
A-375	IC₅₀	0.06 μM Compound: 1	Antiproliferative activity against human A375 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human A375 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27476419]
A-431	IC₅₀	0.2 μM Compound: geldanamycin	Antiproliferative activity against human A431 cells after 72 hrs Antiproliferative activity against human A431 cells after 72 hrs	[PMID: 20655237]
A-431	IC₅₀	40 nM Compound: 1, GA	Cytotoxicity against human A431 cells after 72 hrs by MTT assay Cytotoxicity against human A431 cells after 72 hrs by MTT assay	[PMID: 25277067]
A549	IC₅₀	0.1 μM Compound: GA	Antiproliferative activity against human A549 cells after 72 hrs by SRB assay Antiproliferative activity against human A549 cells after 72 hrs by SRB assay	[PMID: 29172085]
A549	IC₅₀	0.109 μM Compound: Geldanamycin	Anticancer activity against human A549 cells measured after 72 hrs by SRB assay Anticancer activity against human A549 cells measured after 72 hrs by SRB assay	[PMID: 27283788]
A549	IC₅₀	0.15 μM Compound: geldanamycin	Cytotoxicity against human A549 cells after 2 days by AlamarBlue assay Cytotoxicity against human A549 cells after 2 days by AlamarBlue assay	[PMID: 23947794]
A549	IC₅₀	0.99 μM Compound: GDM	Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
A549	IC₅₀	97 nM Compound: 1, GA	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 25277067]
BGC-823	IC₅₀	0.11 μM Compound: 1	Antiproliferative activity against human BGC823 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human BGC823 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27476419]
BGC-823	IC₅₀	40 nM Compound: 1, GA	Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay	[PMID: 25277067]
CAKI-1	IC₅₀	0.056 μM Compound: Geldanamycin	Anticancer activity against human Caki1 cells measured after 72 hrs by SRB assay Anticancer activity against human Caki1 cells measured after 72 hrs by SRB assay	[PMID: 27283788]
CNE2Z	IC₅₀	0.31 μM Compound: GM	Antiproliferative activity against human CNE2Z cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human CNE2Z cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
HCT-116	EC₅₀	0.03 μM Compound: 1	Antiproliferative activity against human HCT116 cells measured on day 4 by Cell titer-glo assay Antiproliferative activity against human HCT116 cells measured on day 4 by Cell titer-glo assay	[PMID: 21420297]
HCT-116	EC₅₀	0.03 μM Compound: 1	Antiproliferative activity against human HCT116 cells by luminescence assay Antiproliferative activity against human HCT116 cells by luminescence assay	[PMID: 21605975]
HCT-116	IC₅₀	0.1 μM Compound: 1	Antiproliferative activity against human HCT116 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human HCT116 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27476419]
HCT-116	IC₅₀	0.15 μM Compound: Geldanamycin	Anticancer activity against human HCT116 cells measured after 72 hrs by SRB assay Anticancer activity against human HCT116 cells measured after 72 hrs by SRB assay	[PMID: 27283788]
HeLa	IC₅₀	>5 μM Compound: Geldanamycin	Cytotoxicity against human HeLa cells at 72 hrs by MTS assay Cytotoxicity against human HeLa cells at 72 hrs by MTS assay	[PMID: 22162786]
HeLa	IC₅₀	0.06 μM Compound: GA	Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay	[PMID: 27266997]
HeLa	IC₅₀	798 nM Compound: 1, GA	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 25277067]
HepG2	IC₅₀	0.3 μM Compound: GDM	Cytotoxicity against human HepG2 cells by MTT assay Cytotoxicity against human HepG2 cells by MTT assay	[PMID: 23656556]
HepG2	IC₅₀	1.74 μM Compound: GM	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
HepG2	IC₅₀	40 nM Compound: 1, GA	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 25277067]
Huh-7	EC₅₀	0.25 nM Compound: Geldanamycin	Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days by qRT-PCR analysis Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days by qRT-PCR analysis	[PMID: 18936191]
Huh-7	EC₅₀	1.2 nM Compound: Geldanamycin	Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 nM HCV-796 and 800 nM boceprevir by qRT-PCR analysis Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 nM HCV-796 and 800 nM boceprevir by qRT-PCR analysis	[PMID: 18936191]
HUVEC	IC₅₀	19 nM Compound: 1, GA	Cytotoxicity against HUVEC cells after 72 hrs by MTT assay Cytotoxicity against HUVEC cells after 72 hrs by MTT assay	[PMID: 25277067]
L02	IC₅₀	141 nM Compound: 1, GA	Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay	[PMID: 25277067]
L6	IC₅₀	6 μM Compound: GA	Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay	[PMID: 24580531]
LNCaP	IC₅₀	0.43 μM Compound: GA	Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay	[PMID: 25105924]
LS174T	IC₅₀	0.45 μM Compound: GA	Cytotoxicity against human LS174T cells by MTS assay Cytotoxicity against human LS174T cells by MTS assay	[PMID: 17034135]
MCF7	GI₅₀	35.6 μM Compound: geldanamycin	Growth inhibition of human MCF7 cells after days by SRB assay Growth inhibition of human MCF7 cells after days by SRB assay	[PMID: 17869098]
MCF7	IC₅₀	0.04 μM Compound: GDA	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay	[PMID: 25075762]
MCF7	IC₅₀	0.0427 μM Compound: 1, GDA	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay	[PMID: 25756299]
MCF7	IC₅₀	0.053 μM Compound: Geldanamycin	Cytotoxicity against human MCF7 cells at 72 hrs by MTS assay Cytotoxicity against human MCF7 cells at 72 hrs by MTS assay	[PMID: 22162786]
MCF7	IC₅₀	0.11 μM Compound: 1	Antiproliferative activity against human MCF7 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human MCF7 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27476419]
MCF7	IC₅₀	9.6 μM Compound: Geldanamycin	Cytotoxicity against human MCF7 cells by SRB assay Cytotoxicity against human MCF7 cells by SRB assay	[PMID: 19560353]
MCF7	IC₅₀	9.8 nM Compound: 5, GDA	Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 72 hrs Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 72 hrs	[PMID: 23648180]
MDA-MB-231	IC₅₀	0.03 μM Compound: GA	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay	[PMID: 27266997]
MDA-MB-231	IC₅₀	0.05 μM Compound: 1, GA	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 25277067]
MDA-MB-231	IC₅₀	0.05 μM Compound: GA	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 25105924]
MDA-MB-231	IC₅₀	0.06 μM Compound: GA	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay	[PMID: 29172085]
MDA-MB-231	IC₅₀	0.11 μM Compound: Geldanamycin	Anticancer activity against human MDA-MB-231 cells measured after 72 hrs by SRB assay Anticancer activity against human MDA-MB-231 cells measured after 72 hrs by SRB assay	[PMID: 27283788]
MDA-MB-231	IC₅₀	0.62 μM Compound: GM	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
NCI-H1975	GI₅₀	0.56 μM Compound: 1; GA	Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells after 1 to 3 days by MTS assay Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells after 1 to 3 days by MTS assay	[PMID: 27783977]
NCI-H1975	GI₅₀	0.56 μM Compound: GA	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by Cell Titer 96 Aqueous One Solution cell proliferation assay Antiproliferative activity against human NCI-H1975 cells after 72 hrs by Cell Titer 96 Aqueous One Solution cell proliferation assay	[PMID: 29202402]
P19	IC₅₀	0.1 μM Compound: 1	Cytotoxicity against mouse P19 cells after 18 hrs Cytotoxicity against mouse P19 cells after 18 hrs	[PMID: 17442565]
PC-3	IC₅₀	0.73 μM Compound: GDM	Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
RPMI-8226	GI₅₀	0.003 μM Compound: Geldanamycin	Growth inhibition of human RPMI8226 cells after 72 hrs by MTS/PMS assay Growth inhibition of human RPMI8226 cells after 72 hrs by MTS/PMS assay	[PMID: 29057043]
Sf9	IC₅₀	74 nM Compound: Geldanamycin	Displacement of GM-BODIPY from human full length HSP90 alpha expressed in baculovirus-infected Sf9 cells after 16 hrs by fluorescence polarization assay Displacement of GM-BODIPY from human full length HSP90 alpha expressed in baculovirus-infected Sf9 cells after 16 hrs by fluorescence polarization assay	[PMID: 24751441]
SK-BR-3	GI₅₀	0.43 μM Compound: 1; GA	Antiproliferative activity against Her2-overexpressing human SKBR3 cells after 1 to 3 days by MTS assay Antiproliferative activity against Her2-overexpressing human SKBR3 cells after 1 to 3 days by MTS assay	[PMID: 27783977]
SK-BR-3	IC₅₀	0.87 μM Compound: GDM	Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
SK-BR-3	IC₅₀	41 nM Compound: GDM	Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay	[PMID: 19405528]
SK-BR-3	IC₅₀	8.5 nM Compound: 5, GDA	Antiproliferative activity against estrogen receptor deficient human SKBR3 cells after 72 hrs Antiproliferative activity against estrogen receptor deficient human SKBR3 cells after 72 hrs	[PMID: 23648180]
SK-OV-3	IC₅₀	0.94 μM Compound: GDM	Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]
SMMC-7721	IC₅₀	0.11 μM Compound: GM	Antiproliferative activity against human SMMC7721 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human SMMC7721 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
SNU-638	IC₅₀	0.03 μM Compound: Geldanamycin	Anticancer activity against human SNU638 cells measured after 72 hrs by SRB assay Anticancer activity against human SNU638 cells measured after 72 hrs by SRB assay	[PMID: 27283788]
SW1990	IC₅₀	0.29 μM Compound: 1	Antiproliferative activity against human SW1990 assessed as reduction in cell viability measured after 96 hrs by MTT assay Antiproliferative activity against human SW1990 assessed as reduction in cell viability measured after 96 hrs by MTT assay	[PMID: 27476419]
SW480	IC₅₀	0.51 μM Compound: GM	Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay	[PMID: 32527461]
SW480	IC₅₀	310 nM Compound: 1, GA	Cytotoxicity against human SW480 cells after 72 hrs by MTT assay Cytotoxicity against human SW480 cells after 72 hrs by MTT assay	[PMID: 25277067]
U-87MG ATCC	EC₅₀	0.089 μM Compound: 1	Antiproliferative activity against human U87 cells by luminescence assay Antiproliferative activity against human U87 cells by luminescence assay	[PMID: 21605975]
U-87MG ATCC	IC₅₀	0.81 μM Compound: GDM	Antiproliferative activity against human U-87 MG cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human U-87 MG cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay	[PMID: 32663707]

In Vitro

Geldanamycin significantly delays and reduces viperin expression, indicating that IRF3 is involved in viperin induction in RAW264.7 cells^[1].
Geldanamycin, a benzoquinone ansamycin, protected against neuronal injury induced by oxygen-glucose deprivation (OGD)/zVAD treatment in cultured primary neurons. More importantly, Geldanamycin decreases RIP1 protein level in a time and concentration-dependent manner. Geldanamycin also decreases the Hsp90 protein level, which causes instability of RIP1 protein, resulting in decreased RIP1 protein level but not RIP1 mRNA level after Geldanamycin treatment^[2].
Geldanamycin is identified as the first natural product inhibitor of Hsp90 that binds to the N-terminal ATPase domain of Hsp90 to inhibit its chaperone function, and significantly induces tumor cell death via an apoptotic mechanism^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvente y solubilidad

In Vitro:

DMSO : 25 mg/mL (44.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7837 mL	8.9184 mL	17.8368 mL
5 mM	0.3567 mL	1.7837 mL	3.5674 mL
10 mM	0.1784 mL	0.8918 mL	1.7837 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.46 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.46 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

Pureza y Documentación

Purity: 99.58%

Ficha de datos (280 KB) SDS (396 KB)

COA (256 KB) HNMR (298 KB) RP-HPLC (223 KB) MS (69 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. 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 [Content Brief]

[2]. Chen WW, et al. RIP1 mediates the protection of Geldanamycin on neuronal injury induced by oxygen-glucosedeprivation combined with zVAD in primary cortical neurons. J Neurochem. 2012 Jan;120(1):70-7. [Content Brief]

[3]. 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. [Content Brief]

[4]. Roe SM, et al. Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin. J Med Chem. 1999 Jan 28;42(2):260-6. [Content Brief]

[5]. Wang C, et al. Geldanamycin Reduces Acute Respiratory Distress Syndrome and Promotes the Survival of Mice Infected with the Highly Virulent H5N1 Influenza Virus. Front Cell Infect Microbiol. 2017 Jun 15;7:267. [Content Brief]

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Geldanamycin [30562-34-6]

Referencia HY-15230-10mg

Contact local distributor :

Marca : MedChemExpress

Contact local distributor :

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