17-DMAG A synthetic Geldanamycin derivative and inhibitor of Hsp90

17-DMAG (CAS 467214-20-6)

17-DMAG | CAS 467214-20-6 is rated 5.0 out of 5 by 1.
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Synonym: 17-Dimethylaminoethylamino-17-demethoxygeldanamycin
Application: A synthetic Geldanamycin derivative and inhibitor of Hsp90
CAS Number: 467214-20-6
Purity: ≥98%
Molecular Weight: 616.75
Molecular Formula: C32H48N4O8
* Refer to Certificate of Analysis for lot specific data (including water content).
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17-DMAG, 17-dimethylaminoethylamino-17-demethoxygeldanamycin, is a synthetic derivative of the antibiotic Geldanamycin (sc-200617) with lower hepatotoxicity than the parent antibiotic and higher potency and availability than the similar derivative 17-AAG (sc-200641). 17-DMAG is described to bind and inhibit the activity of Hsp90 (heat shock protein 90), a cellular chaperone that is over expressed in many cancers, and which participates in folding of proteins found in multiple signal transduction pathways.


References

1. Jez, J.M., et al. 2003. Chem. Biol. 10: 361-368. PMID: 12725864
2. Kaur, G., et al. 2004. Clin. Cancer Res. 10: 4813-4821. PMID: 15269157
3. Hollingshead, M., et al. 2005. Cancer Chemother. Pharmacol. 56: 115-125. PMID: 15791458
4. Gossett, D.R., et al. 2005. Gynecol. Oncol. 96: 381-388. PMID: 15661225

Physical State :
Solid
Solubility :
Soluble in water, ethanol (10 mg/mL), and DMSO (>25 mg/mL).
Storage :
Store at -20° C
Boiling Point :
810.53° C at 760 mmHg
Density :
1.21 g/cm3
Refractive Index :
n20D 1.57
IC50 :
hypoxia-induced HIF1 activation: IC50 = 3.6 nM (human AGS cells); SKBR3 : IC50 = 24 nM (human); HCT-116: IC50 = 57 nM (human); MCF7: IC50 = 71 nM (human)
Ki Data :
Heat shock protein HSP 90-alpha: Ki= 680 nM (human); His-tagged Hsp90: Ki= 250 nM
pK Values :
pKa: 8.48, 9.02
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
5288674
SMILES :
CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)NCCN(C)C)C)OC)OC(=O)N)C)C)O)OC

Download SDS (MSDS)

Certificate of Analysis

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17-DMAG  Product Citations

See how others have used 17-DMAG. Click on the entry to view the PubMed entry .

Citations 1 to 7 of 7 total

PMID: # 24946002  Sun, H. et al. 2014. Br. J. Cancer. 111: 281-91.

PMID: # 22085491  Sobhan, PK. et al. 2012. Cancer Lett. 317: 78-88.

PMID: # 22847000  Narayanan, A. et al. 2012. The Journal of biological chemistry. 287: 33198-214.

PMID: # 19805107  Ayrault, O. et al. 2009. Proc. Natl. Acad. Sci. U.S.A. 106: 17037-17042.

PMID: # 19858214  Zhang, T. et al. 2009. J. Biol. Chem. 284: 35381-35389.

PMID: # 18644871  Bandyopadhyay, U. et al. 2008. Mol. Cell. Biol. 28: 5747-5763.

PMID: # 15542664  Hu, J. et al. 2004. J. Virol. 78: 13122-13131.

Citations 1 to 7 of 7 total
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Rated 5 out of 5 by from Zhang Zhang, T. et al. (PubMed 19858214) used 17-DMAG, a synthetic derivative of Geldanamycin with lower hepatotoxicity, to determine if it inhibits Hsp90-Cdc37 complex formation. While 17-DMAG is highly effective as an inhibitor of Hsp90, it showed no disruption of the Hsp90-Cdc37 complex formation. -SCBT Publication Review
Date published: 2015-02-18
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