半岛bd体育手机客户端 说明
一般描述
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 agentin 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 vitroand an effective anti-angiogenesis agentin vivo(2 to 100 mg/kg in mice and rats; s.c.).
包装
10 mg in Glass bottle
警告
Toxicity: Irritant (B)
其他说明
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C19H28ClNO6 |
分子量 | 401.88 |
半岛bd体育手机客户端 性质
质量水平 | 200 |
测定 | ≥97% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem? |
储存条件 | OK to freeze |
颜色 | white to light yellow |
溶解性 | DMSO: 100 mg/mL |
运输 | ambient |
储存温度 | ?20℃ |
InChI | 1S/C19H28ClNO6/c1-11(2)5-6-13-18(3,27-13)16-15(24-4)12(7-8-19(16)10-25-19)26-17(23)21-14(22)9-20/h5,12-13,15-16H,6-10H2,1-4H3,(H,21,22,23)/t12-,13-,15-,16-,18+,19+/m1/s1 |
InChI key | MSHZHSPISPJWHW-PVDLLORBSA-N |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 2 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |