-
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。
More
-
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。
More
-
MK-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。
More
-
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。
More
-
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.
More
