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。
MoreMK-1775, a potent and selective ATP-competitive inhibitor of WEE1, is cytotoxic across a broad panel of tumor cell lines and induces DNA double-strand breaks. MK-1775是Wee1选择性抑制剂,IC50为5.2 nM,能干扰G2期DNA损伤检查。
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。
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.
MoreFlavopiridol与ATP竞争抑制CDK1,CDK2,CDK4和CDK6,IC50为40 nM。Flavopiridol还具有EGFR和PKA抑制性。
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