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.
PCI-34051是高活性的HDAC8特异性抑制剂,IC50为10 nM,比对其它HDAC亚型的抑制性高200倍以上。
MorePYR-41是特异的可渗透入细胞的泛素激活酶E1抑制剂,IC50< 10 uM,对E2几乎无活性。
MorePD98059是一种非ATP竞争性的MEK抑制剂,IC50为2 μM,特异性抑制MEK-1介导的MAPK激活;不直接抑制ERK1或ERK2。
MorePanobinostat (LBH589)是一种新型的,广谱的HDAC抑制剂,IC50为5 nM。
MoreBIX 02188是一种选择性的MEK5抑制剂,IC50为4.3 nM,也抑制ERK5催化活性,IC50为810 nM,且不抑制与其密切相关的激酶MEK1, MEK2, ERK2,和JNK2。
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