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.
SB-3CT是Gelatinase高效选择性抑制剂,对MMP2和MMP9的Ki值分别为13.9nM和600nM。
MoreFingolimod (FTY720) HCl是一种1-磷酸-神经鞘氨醇S1P受体拮抗剂,IC50为0.33 nM。
MoreCabozantinib (XL184, BMS-907351)是一种有效的VEGFR2抑制剂,在无细胞试验中IC50为0.035 nM,也能有效抑制c-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXL,IC50分别为1.3 nM,4 nM,4.6 nM,12 nM/11.3 nM/6 nM,14.3 nM 和 7 nM。
MoreJNK-IN-8是第一个,不可逆的JNK抑制剂,作用于JNK1, JNK2和JNK3,IC50分别为4.7 nM, 18.7 nM和1 nM,比作用于MNK2, Fms选择性高10倍以上,对c-Kit, Met, PDGFRβ没有抑制作用。
MorePF-543柠檬酸盐是鞘氨醇竞争性的,且可渗透入细胞的SphK1选择性抑制剂,Ki为3.6 nM,对SphK2的抑制性较弱。
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