Entinostat (MS-27-275, MS-275, SNDX-275) an orally class I histone deacetylase (HDAC)-specific inhibitor, is currently in clinical trials.
MoreGW788388, a potent, selective, and orally active inhibitor of TGFβ signaling, shows potent anti-fibrosis effect. GW788388是一种有效的,选择性的ALK5抑制剂,IC50为18 nM,也抑制其他TGF-βI型和II型受体激酶活性,但不抑制BMP II型受体。
MoreRicolinostat (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。
MoreBisindolylmaleimide I (BMI, GF109203X) is a high selectivity, cell-permeable and ATP-competitive inhibitor of PKC and shows GSK-3 inhibition as well. GF 109203X是一种有效的PKC抑制剂,抑制PKCα,PKCβI,PKCβII和PKCγ,IC50分别为20 nM,17 nM,16nM和20 nM,作用于PKC比作用于EGFR,PDGFR和胰岛素受体选择性高3000倍以上。
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。
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