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.
Bisindolylmaleimide 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。
MoreHonokiol, a low molecular weight natural product isolated from the bark of magnolia officinalis, possesses potent anticancer activities which is chiefly via the inhibition of AKT and mitogen-activated protein kinase (MAPK) phosphorylation. Honokiol是木兰的有效成分,抑制Akt磷酸化,且促进ERK1/2磷酸化。
MoreAGI-6780, a heterocyclic urea sulfonamide molecule, potently and selectively inhibits the tumor-associated IDH2 R140Q mutant. AGI-6780 是一种强效的选择性 IDH2 R140Q mutant抑制剂,其IC50为 23 nM。
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