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.
SB216763, a potent and selective cell permeable GSK-3 inhibitor, is equally effective at inhibiting human GSK-3α and GSK-3β. SB216763是一种有效的,选择性GSK-3α抑制剂,IC50为34.3 nM,对GSK-3β具有同样的抑制作用。
MoreDoxycycline盐酸盐是合成的四环素类衍生物,具有抗菌活性。
MoreAZD5363能够有效抑制Akt1/Akt2/3,IC50分别为3 nM/8 nM/8 nM,对P70S6K/PKA也具有相似的抑制效果,对ROCK1/2具有较低的抑制活性。
MoreCO-1686 (AVL-301)是一种不可逆的,突变选择性的EGFR抑制剂,作用于EGFRL858R/T790M和EGFRWT, Ki分别为21.5 nM和303.3 nM。
MoreIniparib (BSI-201)是一种PARP1抑制剂,对三阴性乳腺癌(TNBC)有效。
More