化合物KB-R7943 T6144

Product Introduction
Bioactivity


英文名: KB-R7943 mesylate

描述: KB-R7943 mesylate 是一种广泛使用的反向 Na+/Ca2+ 交换剂 (NCXrev) 抑制剂，IC50 为 5.7±2.1 µM。它通过激活JNK 通路和抑制自噬通量来诱导癌细胞死亡。

细胞实验: Fluorescence microscopy, electrophysiological patch-clamp techniques and cellular respirometry with Seahorse XF24 analyzer were used with cultured hippocampal neurons;?membrane potential imaging, respirometry and Ca(2+) flux measurements were made in isolated rat brain mitochondria[1].

体外活性: KB-R7943 inhibited NCX(rev) with IC(50) = 5.7 ± 2.1 μM, blocked NMDAR-mediated ion currents, and inhibited NMDA-induced increase in cytosolic Ca(2+) with IC(50) = 13.4 ± 3.6 μM but accelerated calcium deregulation and mitochondrial depolarization in glutamate-treated neurons.?KB-R7943 depolarized mitochondria in a Ca(2+) -independent manner.?Stimulation of NMDA receptors caused NAD(P)H oxidation that was coupled or uncoupled from ATP synthesis depending on the presence of Ca(2+) in the bath solution.?KB-R7943, or rotenone, increased NAD(P)H autofluorescence under resting conditions and suppressed NAD(P)H oxidation following glutamate application.?KB-R7943 inhibited 2,4-dinitrophenol-stimulated respiration of cultured neurons with IC(50) = 11.4 ± 2.4 μM.?With isolated brain mitochondria, KB-R7943 inhibited respiration, depolarized organelles and suppressed Ca(2+) uptake when mitochondria oxidized complex I substrates but was ineffective when mitochondria were supplied with succinate, a complex II substrate[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 27 mg/mL (63.16 mM)


关键字: inhibit | KB-R 7943 Mesylate | KB-R-7943 mesylate | KB-R 7943 | Autophagy | KB-R7943 Mesylate | Inhibitor | KB-R-7943 Mesylate | KB R7943 mesylate | Na+/Ca2+ Exchanger | KBR7943 mesylate | KB-R-7943

相关产品: SN 6 | CGP37157 | Terfenadine | SEA0400 | SM-6586 | Benzamil | FR183998 free base | PPADS tetrasodium

相关库: Ion Channel Inhibitor Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Active Compound Library | Autophagy Compound Library | Sodium Channel Blocker Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途