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.
SL-327是可渗透入细胞的MEK-1和MEK-2抑制剂,IC50分别为180nM和220nM。
MoreMEK162(ARRY-438162; ARRY-162)是MEK1/2抑制剂,IC50为12 nM。
MorePimasertib (AS-703026)作用于MM细胞系,是一种高度选择性的,有效的,ATP非竞争性的,MEK1/2变构抑制剂,IC50为0.005-2 μM。
MoreAZD8330是一种新型,选择性的,非ATP竞争性MEK 1/2抑制剂,IC50为7 nM。
MoreRefametinib是口服生物相容性的MEK抑制剂,对MEK1和MEK2的IC50分别为19 nM和47 nM,有抗肿瘤活性。
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