Conglobatin is a dimeric macrolide dilactone originally isolated from S. conglobatus. It disrupts binding of heat shock protein 90 (Hsp90) to the co-chaperone Cdc37 complex and induces downregulation of client protein expression in SK-BR-3 breast cancer cells. It also inhibits cell proliferation in HER2+ breast cancer cell lines (IC50s = 12.9-61.5 uM, respectively) and decreases the number of invasive cells in vitro. When combined with lapatinib , tumor growth of SK-BR-3 mouse xenografts was reduced to a greater degree than with conglobatin alone. Conglobatin has various anticancer effects in esophageal squamous cell carcinoma (ESCC) models as well, including an inhibition of cell proliferation in KYSE510 cells (IC50 = 9.31 uM). It also inhibits β1 integrin activation leading to a loss of cellular adhesion.
Citations
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Chemical Properties
CAS No.
72263-05-9
Chemical Name
(3E,5R,11E)-3,5,7S,11,13R,15S-hexamethyl-8S,16S-bis(5-oxazolylmethyl)-1,9-dioxacyclohexadeca-3,11-diene-2,10-dione
SMILES
C[C@H]([C@H](CC1=CN=CO1)OC(/C(C)=C/[C@H](C)C[C@H](C)[C@H](CC2=CN=CO2)O3)=O)C[C@@H](C)/C=C(C)\C3=O
Molecular Formula
C28H38N2O6
Molecular Weight
498.6
Solubility
DMF: soluble,DMSO: soluble,Ethanol: soluble,Methanol: soluble
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
Reviews
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