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PE859

產(chǎn)品活性：PE859是tau和Aβ積累的有效抑制劑，IC₅₀值分別為0.66 和1.2 μM。

研究領(lǐng)域：Cell Cycle/DNA Damage  |  Cytoskeleton

作用靶點(diǎn)：Microtubule/Tubulin

In Vitro: PE859 inhibits the heparin-induced aggregation of both 3RMBD and full length tau in a concentration-dependent manner. In each assay, the IC₅₀ values calculated at the last measurement periods are 0.81 μM, and 2.23 μM, respectively. PE859 inhibits tau aggregation through formation of beta-sheet structure.

In Vivo: PE859 could cross the blood-brain barrier and that PE859 could be distributed into the tissues of the central nervous system. The maximum concentration of PE859 is 2.005 μg/mL in the blood at 3 h and 1.428 μg/g in the brain at 6 h. PE859 delays onset and progression of the motor dysfunction in JNPL3 mice. PE859 delays progression of the motor dysfunction through the inhibition of accumulation of sarkosyl-insoluble tau.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Anti-Aging Compound Library  |  Cytoskeleton Compound Library  |  Anti-Lung Cancer Compound Library  |  Neurodegenerative Disease-related Compound Library  |  Protein-protein Interaction Inhibitor Library  |  Tirbanibulin dihydrochloride  |  Tubulysin IM-3  |  AMXI-5001 hydrochloride  |  Tubulin polymerization-IN-21  |  Dolastatin 10  |  SB-216  |  MAP4343  |  Tubulin polymerization-IN-8  |  Tubulysin IM-1  |  Colchicine-d₃  |  2-Methoxyestradiol-¹³C,d₃  |  Taltobulin  |  Albendazole  |  Tilavonemab  |  DM4-d₆  |  EGFR-IN-57  |  Epothilone B  |  Epothilone A  |  Maytansinol  |  Docetaxel-d₉  |  Verubulin hydrochloride  |  VcMMAE  |  Tubulin polymerization-IN-15  |  Combretastatin A-1  |  Tubulin/HDAC-IN-1  |  Mc-MMAE  |  7-epi-Taxol  |  Thiocolchicine  |  Fosbretabulin disodium  |  PEG4-aminooxy-MMAF

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