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.

For research use only. We do not sell to patients.

Conglobatin Chemical Structure

Conglobatin Chemical Structure

CAS No. : 72263-05-9

Size Price Stock Quantity
2500 μg USD 2150 Get quote 2 weeks 1 week
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

View All HSP Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

MedChemExpress (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]

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

Structure Classification
Initial Source

Streptomyces conglobatus

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Conglobatin
Cat. No.:
HY-119906
Quantity:
MCE Japan Authorized Agent: