Geldanamycin (NSC 122750) - Moligand™, 10mM in DMSO , Inhibitor of heat shock protein 90 alpha family class B member 1, CAS No.30562-34-6, Inhibitor of heat shock protein 90 alpha family class B member 1

CAS: 30562-34-6 Cat. No.: G408923 Molecular Weight: 560.64 EC Number: 805-356-8

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

2-Azabicyclo[16.3.1]docosa-4,6,10,18,21-pentaene-3,20,22-trione, 9,13-dihydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-, 9-carbamate

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Geldanamycin (NSC 122750) Geldanamycin (NSC 122750) is a natural existing HSP90 inhibitor with K d of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARD
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. 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. 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.

In vivo

Geldanamycin (50 mg//kg) shows 30% inhibition on pl85-associated phosphotyrosine levels in FRE/erbB-2 mice.
Cell Data

cell lines：MDA-MB-468, MCF-7, HCC1954, MDA-MB-231, SKBr-3, Cal-51, and BT-20 breast cancer cells

Concentrations：0.001-10 μM

Incubation Time：3 hours

Powder Purity:≥97%

Specifications

Synonyms

2-Azabicyclo[16.3.1]docosa-4, 6, 10, 18, 21-pentaene-3, 20, 22-trione, 9, 13-dihydroxy-8, 14, 19-trimethoxy-4, 10, 12, 16-tetramethyl-, 9-carbamate

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Geldanamycin (NSC 122750) is a natural existing HSP90 inhibitor with K_d of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respirato

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of heat shock protein 90 alpha family class B member 1

Names and Identifiers

• Isomeric SMILES: C[C@H]1C[C@@H]([C@@H]([C@H](/C=C(/[C@@H]([C@H](/C=C\C=C(\C(=O)NC2=CC(=O)C(=C(C1)C2=O)OC)/C)OC)OC(=O)N)\C)C)O)OC
• WGK Germany: 2
• RTECS: LX8920000
• Alternate CAS: 30562-34-6
• MeSH Entry Terms: geldanamycin;geldanomycin
• Molecular Weight: 560.64
• Reaxy-Rn: 26145919
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26145919&ln=

Associated Targets(Human)

TRAP1 Tchem Heat shock protein 75 kDa, mitochondrial (1 Activities)

Discover Target: TRAP1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HSP90AA1 Tchem Heat shock protein HSP 90-alpha (20 Activities)

Discover Target: HSP90AA1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HSP90AB1 Tchem Heat shock protein HSP 90-beta (8 Activities)

Discover Target: HSP90AB1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 62 mg/mL warmed with 50ºC Water: bath (102.19 mM); Water: Insoluble; Ethanol: Insoluble
• Melt Point(°C): 255°C

References

1. Xu Yao, Jie Zhu, Lin Li, Bo Yang, Bixia Chen, Endong Bao, Xiaohui Zhang.  (2023)  Hsp90 protected chicken primary myocardial cells from heat-stress injury by inhibiting oxidative stress and calcium overload in mitochondria.  BIOCHEMICAL PHARMACOLOGY,      [PMID:36708886] [10.1016/j.bcp.2023.115434]

2. Yuanyuan Zhu, Yanyan Huang, Tian-Hao Yan, Jialuo Li, Yongming Li, Hannah F. Drake, Huifei Zhong, Yulong Jin, Rui Zhao, Hong-Cai Zhou.  (2022)  Metal-Organic Framework-Based Nanoheater with Photo-Triggered Cascade Effects for On-Demand Suppression of Cellular Thermoresistance and Synergistic Cancer Therapy.  Advanced Healthcare Materials,  11  (13): (2200004).  [PMID:35306753] [10.1002/adhm.202200004]