Ricolinostat (ACY-1215) is an oral, first-in-class, selective inhibitor of HDAC6, and inhibits tubulin deacetylase. Rocilinostat (ACY-1215)是高效HDAC6抑制剂,IC50为5 nM,比对HDAC1/2/3的抑制性高10倍以上,对HDAC8有微弱活性,对HDAC4/5/7/9/11,Sirtuin1和Sirtuin2活性最低。
MoreKartogenin (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。
MoreKX2-391 (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。
MorePF-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。
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