A cell-permeable Fumagillin analog that inhibits MetAP2, but not MetAP1, methionine aminopeptidase activity (IC50 = 1nM against human MetAP2), without affecting the inhibitory activity of MetAP2 against HRI- (heme-regulated inhibitor kinase) catalyzed eIF-2alpha phosphorylation. A potent endothelial cytostasis inducer (IC50 = 25 pM and 37 pM, respectively, against HUVEC and bovine BAEC) in vitro and an effective anti-angiogenesis agent in vivo (2-100mg/kg in mice and rats; s.c.).
Formula:C19H28CINO6
Molecular Weight:401.9
Solubility:DMSO (100mg/ml)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
