General description

A cell-permeable Fumagillin (Cat. No. 344845) analog that inhibits MetAP2, but not MetAP1, methionine aminopeptidase activity (IC₅₀ = 1 nM against human MetAP2) by covalently modifying MetAP2 active site histidine (aa 231 in human/mouse/rat; aa 174 in yeast) via its epoxide group, without affecting the inhibitory activity of MetAP2 against HRI- (heme-regulated inhibitor kinase) catalyzed eIF-2α phosphorylation. Cellular MetAP2 inhibition is particularly effective in inducing endothelial cytostasis (IC₅₀ = 25 pM and 37 pM, respectively, against HUVEC and bovine BAEC proliferation by TNP-470), making TNP-470 a potent anti-angiogenesis agent in vivo (2 to 100 mg/kg in mice and rats; s.c.). Reported to be more potent and less toxic than Fumagillin.

A cell-permeable Fumagillin (Cat. No. 344845) analog that inhibits MetAP2, but not MetAP1, methionine aminopeptidase activity (IC₅₀ = 1 nM against human MetAP2), without affecting the inhibitory activity of MetAP2 against HRI- (heme-regulated inhibitor kinase) catalyzed eIF-2α 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 to 100 mg/kg in mice and rats; s.c.).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Zhang, Y., et al. 2000. Proc. Natl. Acad. Sci. USA97, 6427.Sin, N., et al. Proc. Natl. Acad. Sci. USA94, 6099.Yamaoka, M., et al. 1993. Cancer Res.53, 4262.Kusaka, M., et al. 1991. Biochem. Biophys. Res. Commun.174, 1070.Ingber, D., et al. 1990. Nature348, 555.

Packaging

10 mg in Glass bottle

Warning

Toxicity: Irritant (B)