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.
GW788388, a potent, selective, and orally active inhibitor of TGFβ signaling, shows potent anti-fibrosis effect. GW788388是一种有效的,选择性的ALK5抑制剂,IC50为18 nM,也抑制其他TGF-βI型和II型受体激酶活性,但不抑制BMP II型受体。
MoreRicolinostat (ACY-1215) is an oral, first-in-class, selective inhibitor of HDAC6, and inhibits tubulin deacetylase. Rocilinostat (ACY-1215)是高效HDAC6抑制剂,IC50为5 nM,比对HDAC1/2/3的抑制性高10倍以上,对HDAC8有微弱活性,对HDAC4/5/7/9/11,Sirtuin1和Sirtuin2活性最低。
MoreBisindolylmaleimide I (BMI, GF109203X) is a high selectivity, cell-permeable and ATP-competitive inhibitor of PKC and shows GSK-3 inhibition as well. GF 109203X是一种有效的PKC抑制剂,抑制PKCα,PKCβI,PKCβII和PKCγ,IC50分别为20 nM,17 nM,16nM和20 nM,作用于PKC比作用于EGFR,PDGFR和胰岛素受体选择性高3000倍以上。
MoreStemRegenin 1 (SR1), a purine derivative, is a high affinity antagonist of the aryl hydrocarbon receptor (AhR) transcription factor that expands CD34+ cells. StemRegenin 1(SR1)是芳香烃受体(AhR)拮抗剂,能促进人CD34+外周血和脐带血造血干细胞(HSC)的自我更新。
MoreNicotinamide (NAM), an amide form of niacin (vitamin B3), is a water-soluble and noncompetitive inhibitor of the deacetylation reaction catalyzed by Sirtuins and it acts as constituent of the enzyme cofactors NAD and NADP. Nicotinamide (Vitamin B3) 是一种水溶性维生素,是NAD 和 NADP的活性成分,也是一种sirtuins抑制剂。
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