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.
nor-NOHA dihydrochloride 是一种选择性的,可逆的 arginase 抑制剂。nor-NOHA dihydrochloride 在缺氧条件诱导 ARG2 表达细胞的 apoptosis。nor-NOHA dihydrochloride 有抗白血病的活性。nor-NOHA dihydrochloride 可用于研究内皮功能障碍、免疫抑制及代谢
MoreNavoximod (GDC-0919, NLG-919) 是一种有效的 IDO(indoleamine-(2,3)-dioxygenase) 途径的抑制剂,其Ki值为7 nM,EC50值为75 nM。
MoreEpacadostat (INCB 024360) 是一种有效,选择性的 IDO1 抑制剂, IC50 为 71.8 nM。Epacadostat 可有效降低色氨酸代谢,增加树突状细胞的活化和成熟,增强效应 T 细胞和自然杀伤细胞的增殖,减弱 Treg 细胞扩增
MoreA-485 是一种化学探针,是 p300/CBP 的强效选择性催化抑制剂,对 p300 和 CBP 组蛋白乙酰转移酶 (HAT) 的 IC50 值分别为 9.8 nM 和 2.6 nM
MoreGSK126 (GSK2816126A, GSK2816126) 是一种有效的,高选择性EZH2 methyltransferase抑制剂,IC50为9.9 nM,对 EZH2 的选择性比其他20种人甲基转移酶高1000多倍。
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