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.
A-674563是Akt1抑制剂,IC50为14 nM,还能抑制PKA和CDK2,IC50分别为16和46 nM。
More17-DMAG (Alvespimycin) HCl是一种水溶性HSP90抑制剂,IC50为62 nM。
MoreRepSox是一种选择性TGFβ/ALK5抑制剂,抑制ATP与ALK5结合以及ALK5自磷酸化时, IC50分别为23 nM和4 nM。
MorePerifosine (KRX-0401)是一种新型的Akt抑制剂,IC50为4.7 μM,靶向作用于Akt的pleckstrin homology (PH)区。
MoreGDC-0068(RG 7440)是泛Akt抑制剂,对Akt1/2/3的IC50分别为5 nM/18 nM/8 nM,比对PKA的抑制性高620倍。
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