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.
HO-3867, an analog of curcumin, is a selective STAT3 inhibitor.
MoreWP1066是一种新型JAK2和STAT3抑制剂,IC50分别为2.30 μM和2.43 μM;对JAK2, STAT3, STAT5和ERK1/2具有抑制活性,但不抑制JAK1和JAK3。
MoreRo 31-8220(Bisindolylmaleimide IX)甲磺酸盐是泛PKC抑制剂,对PKC-α,PKC-βI,PKC-βII,PKC-γ和PKC-ε的IC50分别为5 nM,24 nM,14 nM,27 nM和24 nM。
MoreCPI-613是Lipoate类似物,抑制线粒体酶pyruvate dehydrogenase (PDH)(丙酮酸脱氢酶)和α-ketoglutarate dehydrogenase(α-酮戊二酸脱氢酶),干扰肿瘤细胞线粒体代谢。
MoreLinagliptin是高活性DPP-4抑制剂,IC50为1 nM,对hERG的亲和力较低。
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