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.
RGFP966是一种HDAC抑制剂,作用于HDAC3的IC50为0.08μM ,比作用于其他HDAC选择性高200倍以上。
MoreQNZ (EVP4593)有效抑制NF-κB激活和TNF-α产生,IC50分别为11 nM和7 nM。
MoreAT13148是口服的多AGC激酶抑制剂,有很好的抗肿瘤活性,是AKT,p70S6K,PKA,ROCK和SGK抑制剂。
MorePirfenidone抑制TGF-β产生和TGF-β刺激的胶原蛋白产生,且降低TNF-α和IL-1β产量,具有抗纤维化和抗炎特性。
MoreGo 6983是一种pan-PKC抑制剂,作用于PKCα, PKCβ, PKCγ和PKCδ,IC50分别为7 nM, 7 nM, 6 nM和10 nM,对PKCζ作用稍弱,抑制PKCμ活性。
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