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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。
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Kartogenin (KGN), a small molecular compound, can induce bone marrow-derived mesenchymal stem cells (BMSCs) into chondrocytes. Kartogenin是针对软骨形成的小分子激动剂，促进软骨细胞分化（EC50为100nM），结合filamin A，并阻止其与转录因子CBFβ)的相互作用。
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KX2-391 (KX-01), the first peptidomimetic Src kinase inhibitor, is a synthetic, orally bioavailable inhibitor that has tubulin polymerization inhibition as a second mechanism of action, and is currently in Phase-2 testing for solid tumors. KX2-391 (KX01)是第一个进入临床的拟肽类Src抑制剂，靶向Src的多肽底物结合位点，对多种癌细胞株GI50为9-60 nM。
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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。
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PF-562271, which is a potent ATP-competitive Pyk2/FAK dual inhibitor, has completed phase I clinical trial and is considered to be a promising drug for patients with solid tumors. PF-562271是一种有效的，ATP竞争性的，可逆的FAK抑制剂，IC50为1.5 nM，作用于Pyk2比作用于FAK选择性低10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。
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