In some cases, receptor activation caused by ligand binding to a receptor is directly coupled to the cell's response to the ligand. For example, the neurotransmitter GABA can activate a cell surface receptor that is part of an ion channel. GABA binding to a GABAA receptor on a neuron opens a chloride-selective ion channel that is part of the receptor. GABAA receptor activation allows negatively charged chloride ions to move into the neuron, which inhibits the ability of the neuron to produce action potentials.
Z-VAD-FMK是一种可渗透细胞的,不可逆的pan-caspase抑制剂,能够抑制细胞凋亡。
MoreMM-102是一种有效的WDR5/MLL相互作用抑制剂, WDR5结合检测中, IC50 =2.4 nM, Ki < 1nM。
MoreCathepsin Inhibitor 1是一种组织蛋白酶(L, L2, S, K, B)的抑制剂, pIC50分别为7.9, 6.7, 6.0, 5.5, 5.2。
MoreNeratinib (HKI-272)是一种高度选择性的HER2和EGFR抑制剂,IC50分别为59 nM和92 nM;微弱抑制KDR和Src,对Akt,CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf和c-Met没有显著的抑制作用。
MoreQuisinostat (JNJ-26481585)是一种新型的,二代HDAC抑制剂,对HDAC作用最有效,IC50为0.11 nM,适度有效作用于HDACs 2, 4, 10,和11;比作用于HDACs 3, 5, 8,和9选择性强30倍,对HDACs 6和7作用效果最弱。
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