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.
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)。
MoreSelumetinib (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。
MoreSodium phenylbutyrate (NaPB), a derivative of the short-chain fatty acid butyrate, is a low-potency histone deacetylase inhibitor and originally approved for treatment of UCD. Sodium Phenylbutyrate是一种转录调节因子,通过调控HDAC活性来改变染色质结构从而发挥作用,是组蛋白脱乙酰酶(HDAC)抑制剂,IC50为1-5 uM。
MorePazopanib, an orally available multi-kinase inhibitor of VEGFR, PDGFR, KIT, FGFR, as well as RAF, shows potent activity against a variety of solid tumors. Pazopanib是多重靶点抑制剂,对VEGFR1, VEGFR2,VEGFR3,PDGFR,FGFR,c-Kit 和 c-Fms的IC50分别为10 nM,30 nM,47 nM,84 nM,74 nM,140 nM和146 nM。
MoreDoramapimod (BIRB 796)是高度选择性p38α MAPK抑制剂,Kd为0.1 nM,对JNK2,c-RAF,Fyn,Lck,ERK-1,SYK,IKK2,ZAP-70,EGFR,HER2,PKA,PKC和PKCα/β/γ的抑制性较弱。
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