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.
Nicotinamide (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。
MoreMG-101是一种有效的半胱氨酸蛋白酶抑制剂, 作用于钙蛋白酶I, 钙蛋白酶II, 组织蛋白酶B, 和组织蛋白酶L, Ki值分别为190 nM , 220 nM, 150 nM, 500 pM.
MoreCryptotanshinone是一种STAT3抑制剂,抑制STAT3 Tyr705磷酸化,对STAT3 Ser727作用效果弱,对STAT1和STAT5没有作用效果。
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