product name Fumagillin
Description: Fumagillin is a selective and potent irreversible inhibitor of Methionine aminopeptidase 2 (MetAP2), it is primarily used as an antibiotic to treat microsporidiosis. Fumagillin is a complex natural product antibiotic which covalently binds a key histidine residue of methionine aminopeptidase type II (MetAP-2), inhibiting endothelial cell proliferation and angiogenesis. Fumagillin selectively inhibits the growth of a Δmap1 strain but not a wild-type or a Δmap2 S. cerevisiae strain missing MetAP-2.
References: Proc Natl Acad Sci U S A. 1997 Jun 10;94(12):6099-103; World J Gastroenterol. 2005 Feb 14;11(6):771-7.
458.54
Formula
C26H34O7
CAS No.
23110-15-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 92 mg/mL (200.6 mM)
Water: <1 mg/mL
Ethanol: 32 mg/mL (69.8 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Fumagillin selectively inhibits the growth of a Δmap1 strain but not a wild-type or a Δmap2 S. cerevisiae strain missing MetAP-2. In budding yeast cells, as a potent inhibitor of angiogenesis, Fumagillin not only reverses the growth inhibitory activity of Vpr, but also inhibits Vpr-dependent viral gene expression upon the infection of human macrophages. Though the toxicity of fumagillin has limited its use for human applications, the analogues using structure-activity relationships relating to its angiogenesis properties may be further explored in the treatment of angiogenesis-dependent diseases. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In DEN-treated rats, fumagillin (30 mg/kg, i.p.) inhibits both progression of HCC in the liver itself and systemic metastasis. |
| Animal model | |
| Formulation & Dosage | |
| References | Proc Natl Acad Sci U S A. 1997 Jun 10;94(12):6099-103; World J Gastroenterol. 2005 Feb 14;11(6):771-7. |
