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Signal Pathway


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.

  • CX-4945 EY0441

    CX-4945 (Silmitasertib), a selective, potent and orally bioavailable inhibitor of potent casein kinase II (CK2), is the first small molecule inhibitor of CK2 to progress to human clinical trials. CX-4945 (Silmitasertib)是高活性ATP竞争性CK2抑制剂，对重组型人CK2α的Ki和IC50分别为0.38和1 nM。

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  • Anisomycin EY0446

    Anisomycin, a bacterial antibiotic, known as a peptidyl transferase inhibitor, induces apoptosis by activating several MAPKs and by inhibiting protein synthesis. Anisomycin是一种吡咯烷抗生素, 抑制蛋白质合成, 也是有效的SAPKs/JNKs激活剂。

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  • BI-D1870 EY0449

    BI-D1870是ATP竞争性S6核糖体抑制剂，对RSK1/2/3/4的IC50分别为31 nM/24 nM/18 nM/15 nM，比对MST2，GSK-3β，MARK3，CK1 和Aurora B的抑制性高10到100倍。

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  • Tubastatin A HCl EY0452

    Tubastatin A盐酸盐是HDAC6选择性抑制剂，IC50为15 nM，比对其它亚型的抑制性高1000倍（相对HDAC8是57倍）。

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  • Selumetinib EY0454

    Selumetinib (AZD6244)是一种高选择性的MEK1抑制剂，IC50为14 nM，也抑制ERK1/2磷酸化，IC50为10 nM，但对p38α， MKK6， EGFR， ErbB2， ERK2， B-Raf等没有抑制作用。

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