(E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE C화학적 특성, 용도, 생산
개요
FK-
866 is a highly specific non-
competitive inhibitor of Nampt (K
i = 0.4 nM), causing gradual NAD
+ depletion. In HepG2 human liver carcinoma cells, NAD
+ depletion by FK-
866 directs delayed cell death by apoptosis (IC
50 = ~1 nM). In normal human smooth muscle cells, FK-
866 causes premature senescence, an effect that may be linked to decreased activity of the NAD
+-
dependent enzyme SIRT1. Also, FK-
866 induces autophagy in SH-
SY5Y neuroblastoma cells, as indicated by the formation of LC3-
positive vesicles.
용도
FK866 hydrochloride hydrate has been used:
- to investigate its effects on intra-axonal NAD+ levels
- to induce NAD+ depletion
- to reduce the level of tumor necrosis factor-α (TNF-α), nicotinamide phosphoribosyltransferase (NAMPT) and interleukin-6 (IL-6) in the ischemic brain tissue
일반 설명
A cell-permeable pyridinylacrylamide compound that acts as a selective, allosteric NAPRT/NAMPT (nicotinamide phosphoribosyltransferase) inhibitor (K
i = 0.4 nM for the enzyme/substrate complex; K
i′ = 0.3 nM for the free enzyme), while exhibiting no effect toward NPRT (nicotinic acid phosphoribosyltransferase) activity (82% inhibition of NAPRT activity at 10 nM vs no inhibition of NPRT activity at 1 μM in K-562 extract). FK866 treatment is shown to induce cell death by depleting NAD
+ (Cat. Nos. 481911 & 481915) in HepG2 and NIH-3T3 cultures (by >95% after 24 h treatment of 10 nM FK866), likewise the addition of exogenous NAD
+ is demonstrated to rescue NIH-3T3 and SH-SY5Y from FK866-induced NAD
+-depletion and cell death.
(E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE 준비 용품 및 원자재
원자재
준비 용품
