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Geldanamycin [Hsp90 Inhibitor]

[CAT#: MOD2005ZP96]

Selective Hsp90 inhibitor. Breast cancer stem cell inhibitor.

Target:
HSP90 alpha

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Description
Selective Hsp90 inhibitor. It also a pp60src tyrosine kinase inhibitor and an effective nuclear hormone receptor family inhibitor. Inhibit c-myc gene expression and inhibit abl, erbB, fps, src and yes transformation activity. Destroy the stability of several oncogene and proto-oncogene products. Inhibits breast cancer stem cells. Show effective anti-tumor activity.
Modulator Type
Inhibitor
Relevant Disease
Neurological Disorders
Assay Description
Geldanamycin can significantly delay and reduce viperin expression, indicating that IRF3 is involved in the induction of viperin in RAW264.7 cells [1]. Geldanamycin (GA) is benzoquinone ansamycin, which is protected from neuronal damage induced by oxygen glucose deprivation (OGD)/zVAD treatment in cultured primary neurons. Geldanamycin is shown to reduce RIP1 protein levels in a time- and concentration-dependent manner. Geldanamycin also reduces Hsp90 protein levels, resulting in instability of RIP1 protein, resulting in decreased RIP1 protein levels after geldanamycin treatment, but reduced RIP1 mRNA levels [2]. Geldanamycin (GA) is identified as the first natural product Hsp90 inhibitor, which binds to the N-terminal ATPase domain of Hsp90 to inhibit its chaperone function and significantly induces tumor cell death through an apoptosis mechanism [3].
Reference
[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

[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.

[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.
Molecular Weight
560.6
Form
Powder
Chemical Formula
C29H40N2O9
Source
Synthetic
SMILES
O=C1C(OC)=C(C[C@@H](C)C[C@H](OC)[C@H](O)[C@@H](C)/C=C(C)/[C@H](OC(N)=O)[C@@H](OC)/C=C/C=C(C)/C2=O)C(C(N2)=C1)=O
IC50
1.2 μM
CAS NO.
30562-34-6
PubChem Substance ID
13017912
Purity
>98%
Shipping
Room Temperature
Handling Advice
For obtaining a higher solubility, please warm the tube at 37 °C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -31°C for several months.
Research Use Only
For research use only
Target
HSP90 alpha
Official Name
Hsp90
Full Name
heat shock protein 90
Alternative Names
HATPase
Gene ID
3326(Human); 15516(Mouse); 301252(Rat)
Uniprot ID
P08238(Human); P11499(Mouse); P34058(Rat)
For Research Use Only. Not For Clinical Use.
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