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.
TWS119是一种GSK-3β抑制剂,IC50为30 nM;能够诱导神经细胞的分化,有助于干细胞生物学的研究。
MoreXAV-939能够通过抑制tankyrase1/2而选择性抑制Wnt/β-catenin介导的转录,IC50分别为11 nM/4 nM,对CRE, NF-κB和TGF-β无抑制作用。
MoreTenofovir能阻断HIV-1和HBV的逆转录酶,对HIV-1和HIV-2的IC50分别为0.5-2.2 uM和1.6-4.9 uM。
MoreErlotinib (厄洛替尼; OSI-744; NSC 718781; R1415) 是EGFR抑制剂,IC50为2 nM,比对人c-Src和v-Abl的抑制性高1000倍以上。
MoreEnzastaurin (LY317615)是PKCβ选择性抑制剂,IC50为6 nM,比对PKCα,PKCγ和PKCε的抑制性强6-20倍。
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