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KB-R7943 mesylate
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KB-R7943 mesylate
CAS No. : 182004-65-5
MCE 站:KB-R7943 mesylate
产品活性:KB-R7943 mesylate 是一种 Na+/Ca2+ 交换体 (NCXrev) 反向抑制剂,IC50 为 5.7±2.1 ?M。KB-R7943 mesylate 通过激活JNK通路和抑制自噬通量来诱导癌细胞死亡.
研究领域:Membrane Transporter/Ion Channel | Autophagy
作用靶点:Na+/Ca2+ Exchanger | Autophagy
In Vitro: KB-R7943 mesylate blocks NMDAR-mediated ion currents, and inhibits NMDA-induced increase in cytosolic Ca2+ with IC50=13.4±3.6 ?M but accelerates calcium deregulation and mitochondrial depolarization in glutamate-treated neurons. KB-R7943 depolarizes mitochondria in a Ca2+-independent manner. KB-R7943 inhibits 2,4-dinitrophenol-stimulated respiration of cultured neurons with IC50=11.4±2.4 ?M. In addition to NCXrev, KB-R7943 dose-dependently and reversibly blocked ion currents elicited by NMDA. KB-R7943 dose-dependently inhibits NMDA-induced increases in [Ca2+]c with IC50=13.4±3.6 ?M confirming the inhibition of NMDA receptors observed in electrophysiological experiments. wtRyR1-HEK 293 pretreated with KB-R7943 (10 μM, 10 min) dissolved in the bulk perfusion exhibited significantly attenuated responses to caffeine. In this regard, KB-R7943 produced more pronounced inhibition of caffeine-induced Ca2+ release elicited by 1 mM compared with 0.5 and 0.75 mM (60 versus 58 versus 37%, p<0.05, respectively). KB-R7943 inhibits both IhERG and native IKr rapidly on membrane depolarization with IC50 values of ~89 and ~120 nM, respectively, for current tails at ?40 mV following depolarizing voltage commands to +20 mV. IhERG inhibition by KB-R7943 exhibits both time- and voltage-dependence but shows no preference for inactivated over activated channels.
相关产品:Bioactive Compound Library Plus | Membrane Transporter/Ion Channel Compound Library | Anti-Cancer Compound Library | Autophagy Compound Library | CGP37157 | Terfenadine | SEA0400 | Benzamil hydrochloride | PPADS tetrasodium | ORM-10962 | SN 6 | SM-6586 | YM-244769 dihydrochloride | Caldaret
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