Chemical Name: 2-[(1R)-1-[[(4-Chlorophenyl)sulfonyl](2,5-difluorophenyl)amino]ethyl-5-fluorobenzenebutanoic acid
Biological ActivityOrally active, potent γ-secretase inhibitor (IC50 = 12 nM). Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo. Exhibits no Notch toxicity. Brain penetrant.
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Dynamics of β-Amyloid reductions in brain, cerebrospinal fluid, and plasma of β-amyloid precursor protein transgenic mice treated with a γ-secretase inhibitor.
Barten et al.
Reductions in β-amyloid concentrations in vivo by the γ-secretase inhibitors BMS-289948 and BMS-299897.
Anderson et al.
Ex vivo occupancy of the γ-secretase inhibitors correlates with brain β-amyloid peptide reduction in Tg2576 mice.
Goldstein et al.
Citations for BMS 299897
The citations listed below are publications that use Tocris products. Selected citations for BMS 299897 include:
2 Citations: Showing 1 - 2
APP upregulation contributes to retinal ganglion cell degeneration via JNK3.
Authors: Liu Et al.
Cell Death Differ 2018;25:661
Neuroprotective astrocyte-derived Ins/IGF-1 stimulates endocytic processing and extracellular release of neuron-bound Aβ oligomers.
Authors: Pitt Et al.
Mol Biol Cell 2017;28:2623
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gamma -secretase (100 nM BMS 299897 and 250 nM DAPT)
Using more specific inhibitors, we ruled out the involvement of gamma -secretase (100 nM BMS 299897 and 250 nM DAPT) or matrix metalloproteinases 1, 2, 3, 7, 9, 14, and 17 (0.1–1 μM batimastat and marimastat), as their inhibitors failed to alter A beta O release