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.
MG-101是一种有效的半胱氨酸蛋白酶抑制剂, 作用于钙蛋白酶I, 钙蛋白酶II, 组织蛋白酶B, 和组织蛋白酶L, Ki值分别为190 nM , 220 nM, 150 nM, 500 pM.
MoreCryptotanshinone是一种STAT3抑制剂,抑制STAT3 Tyr705磷酸化,对STAT3 Ser727作用效果弱,对STAT1和STAT5没有作用效果。
MoreGSK343是一种选择性EZH2抑制剂,IC50为4 nM,比作用于EZH1选择性高60倍,比作用于其他组蛋白甲基转移酶选择性高1000倍以上。
MoreEX 527 (Selisistat)是一种有效的,选择性的SIRT1抑制剂,IC50为38 nM,比作用于SIRT2和SIRT3选择性高200倍以上。
MoreNiclosamide, an FDA approved anthelmintic drug, is an inhibitor of Wnt co-receptor LRP6 and suppresses both the Wnt/β-catenin pathways and the mTOR/STAT3 pathway. Niclosamide抑制DNA复制,抑制STAT,IC50为0.7 μM。
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