An Hsp90 inhibitor
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Conglobatin

Item No. 21766

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal 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
CAS Number
72263-05-9
Molecular Formula
C28H38N2O6
Formula Weight
498.6
Purity
≥85%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: SolubleDMSO: SolubleEthanol: SolubleMethanol: Soluble
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
InChi Code
InChI=1S/C28H38N2O6/c1-17-7-19(3)25(11-23-13-29-15-33-23)35-28(32)22(6)10-18(2)8-20(4)26(12-24-14-30-16-34-24)36-27(31)21(5)9-17/h9-10,13-20,25-26H,7-8,11-12H2,1-6H3/b21-9-,22-10+/t17-,18-,19+,20+,25+,26+/m1/s1
InChi Key
LAJRJVDLKYGLOO-ZOMHODHKSA-N
Origin
Bacterium/Streptomyces conglobatus
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $224

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    2.5 mg

    $1,006

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    Cayman Chemical
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    Product Description

    Conglobatin is a dimeric macrolide dilactone originally isolated from S. conglobatus.1 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.2 It also inhibits cell proliferation in HER2+ breast cancer cell lines (IC50s = 12.9-61.5 µM, respectively) and decreases the number of invasive cells in vitro.2,3 When combined with lapatinib (Item No. 11493), tumor growth of SK-BR-3 mouse xenografts was reduced to a greater degree than with conglobatin alone.4 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 µM).5 It also inhibits β1 integrin activation leading to a loss of cellular adhesion.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Westley, J.W., Liu, C.-M., Evans, R.H., et al. Conglobatin, a novel macrolide dilactone from Streptomyces conglobatus ATCC 31005. J. Antibiot. (Tokyo) 32(9), 874-877 (1979).

    2. Huang, W., Ye, M., Zhang, L.-r., et al. FW-04-806 inhibits proliferation and induces apoptosis in human breast cancer cells by binding to N-terminus of Hsp90 and disrupting Hsp90-Cdc37 complex formation. Mol. Cancer. 13, 150 (2014).

    3. Najumudeen, A.K., Jaiswai, A., Lectez, B., et al. Cancer stem cell drugs target K-ras signaling in a stemness context. Oncogene 35(40), 5248-5262 (2016).

    4. Huang, W., Wu, Q.-d., Zhang, M., et al. Novel Hsp90 inhibitor FW-04-806 displays potent antitumor effects in HER2-positive breast cancer cells as a single agent or in combination with lapatinib. Cancer Lett. 356(2 Pt B), 862-871 (2015).

    5. Li, L.-Y., Jiang, H., Xie, Y.-M., et al. Macrolide analog F806 suppresses esophageal squamous cell carcinoma (ESCC) by blocking β1 integrin activation. Oncotarget 6(18), 15940-15952 (2015).