The JAK-STAT signaling pathway transmits information from extracellular chemical signals to the nucleus resulting in DNA transcription and expression of genes involved in immunity, proliferation, differentiation, apoptosis and oncogenesis. The JAK-STAT signalling cascade consists of three main components: a cell surface receptor, a Janus kinase (JAK) and two Signal Transducer and Activator of Transcription (STAT) proteins. Disrupted or dysregulated JAK-STAT functionality can result in immune deficiency syndromes and cancers.
SD-208是口服活性的ATP竞争性TGF-βRI抑制剂,IC50为49 nM,比对TGF-βRII和其它激酶的抑制性高100倍和17倍。
MorePD318088是ATP非竞争性MEK1/2变构抑制剂,能与ATP同时结合于MEK1,且其结合位点与ATP结合位点相邻。
MoreTAK-733是MEK变构抑制剂,对MEK1的IC50为3.2 nM,而对Abl1,AKT3,c-RAF,CamK1,CDK2和c-Met则无活性。
MoreCobimetinib是MEK1/2高选择性抑制剂。
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