1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
    Apoptosis
  2. HSP
    Apoptosis
  3. Conglobatin

Conglobatin (Synonyms: FW-04-806)

Cat. No.: HY-119906
Handling Instructions

Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo.

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Conglobatin Chemical Structure

Conglobatin Chemical Structure

CAS No. : 72263-05-9

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Description

Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo[1][2][3].

IC50 & Target[2]

HSP90

 

In Vitro

Conglobatin (6.25-100 μM; 48 h) markedly inhibits the proliferation of SKBR3 and MCF-7 cells, with IC50s of 12.11 and 39.44 μM, respectively[2].
Conglobatin inhibits cell proliferation in EC109, KYSE70, KYSE450, KYSE150, KYSE180, and KYSE510 cells, with IC50s of 16.43, 15.89, 10.94, 10.50, 10.28, and 9.31 μM, respectively[3].
Conglobatin (10-40 μM; 24 h) displays obvious arrest of SKBR3 and MCF-7 cells in the G2/M phase. Conglobatin induces apoptosis through caspase-dependent pathways in SKBR3 and MCF-7 cells[2].
Conglobatin (10-40 μM; 3-24 h) reduces Hsp90 client protein levels and induces proteasome-dependent degradation[2].
Conglobatin binds to the N-terminal of Hsp90, does not affect ATP-binding capability of Hsp90, but inhibits Hsp90/Cdc37 chaperone/co-chaperone interactions[2].

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

Cell Proliferation Assay[2]

Cell Line: SKBR3 and MCF-7 cells
Concentration: 6.25, 12.5, 25, 50, 100 μM
Incubation Time: 48 hours
Result: Inhibited the proliferation of SKBR3 and MCF-7 cells in a dose-dependent manner.

Cell Cycle Analysis[2]

Cell Line: SKBR3 and MCF-7 cells
Concentration: 10, 20, 40 μM
Incubation Time: 24 hours
Result: Increased the G2/M cell population and decreased the population in the S and G0/G1 phases.

Western Blot Analysis[2]

Cell Line: SKBR3 and MCF-7 cells
Concentration: 10, 20, 40 μM
Incubation Time: 3, 6, 12, 24 hours
Result: Decreased the levels of the client proteins HER2, p-HER2, Raf-1, Akt, and p-Akt in a dose and time-dependent manner in SKBR3 cells.
Reduced the the levels of the client proteins Raf-1, Akt, and p-Akt in a dose and time-dependent manner in MCF-7 cells.
In Vivo

Conglobatin (50-200 mg/kg; i.g. q3d for 24 d) inhibits the tumor growth of SKBR3 and MCF-7 human breast cancer xenograft models in a dose-dependent manner[2].
Conglobatin (4-8 mg/kg; i.p. daily for 21 days) inhibits tumor growth in EC109 and KYSE510 tumor xenograft models with low toxicity[3]

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

Animal Model: BALB/c (nu/nu) athymic mice with SKBR3 and MCF-7 tumor xenograft[2]
Dosage: 50, 100, 200 mg/kg
Administration: Oral gavage every 3 days for 24 days
Result: Showed inhibition of tumor growth at a rate of 39.1%, 52.7%, and 67.5% in the SKBR3 cell line groups and 27.3%, 39.8%, 54.3% in the MCF-7 cell line groups at the three increasing doses, respectively.
Was well tolerated.
Molecular Weight

498.61

Formula

C₂₈H₃₈N₂O₆

CAS No.
SMILES

C[[email protected]@H](C[[email protected]](/C=C(C(O[[email protected]]1CC2=CN=CO2)=O)\C)C)[[email protected]@H](OC(/C(C)=C/[[email protected]@H](C[[email protected]@H]1C)C)=O)CC3=CN=CO3

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

ConglobatinFW-04-806HSPApoptosisHeat shock proteinsmacrolidedilactoneStreptomycesconglobatusHsp90breastcanceresophagealsquamouscellcarcinomaantitumorInhibitorinhibitorinhibit

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