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。
MoreCalcitriol, the active form of vitamin D, is known for its anticancer properties including induction of apoptosis as well as the inhibition of angiogenesis and metastasis.Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol )是维生素D3的活性代谢物,能激活维生素D受体(VDR)。
MoreNicotinamide (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。
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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