Benutzer:Gunnar Römer/Testseite
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| In vitro Activity [1][2] | |
|---|---|
| Probe name | BI 99179 |
| Inhibition of FASN* (IC50) [nM] | 79 |
| Inhibition of [14C]acetate incorporation§ mouse N-42 cells (IC50) [nM] | 570 |
| Inhibition of [14C]acetate incorporation§ hum. H1975 cells (IC50) [nM] | 180 |
| Cytotoxicity (LDH release from U937 cells) (IC50) [nM] | >30000 |
| *Human FAS enzyme isolated from HeLa cells.
§Cells incubated with compound for 1 hour,14C-acetate in Krebs-Ring buffer incubation FASN, fatty acid synthase; LDH, lactate dehydrogenase. |
| In vitro Activity [1][2] | |
|---|---|
| Probe name | BI 99179 |
| Inhibition of FASN* (IC50) [nM] | 79 |
| Inhibition of [14C]acetate incorporation§ mouse N-42 cells (IC50) [nM] | 570 |
| Inhibition of [14C]acetate incorporation§ hum. H1975 cells (IC50) [nM] | 180 |
| Cytotoxicity (LDH release from U937 cells) (IC50) [nM] | >30000 |
| *Human FAS enzyme isolated from HeLa cells.
§Cells incubated with compound for 1 hour,14C-acetate in Krebs-Ring buffer incubation FASN, fatty acid synthase; LDH, lactate dehydrogenase. | |
- ↑ a b Kley JT, Mack J, Hamilton B, Scheuerer S, Redemann N. Discovery of BI 99179, a potent and selective inhibitor of type I fatty acid synthase with central exposure. Bioorg Med Chem Lett 2011, 21, 5924-5927. doi:10.1016/j.bmcl.2011.07.083, PubMed
- ↑ a b Link to molecule page on the NME OI Portal [Portal name] (Will be submitted later)