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  • KX2-391 EY0397

    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 EY0367

    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 EY0368

    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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  • Honokiol EY0371

    Honokiol, 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。

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  • MG-101 EY0341

    MG-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.

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