TGF-betaR1(ALK5)
Transforming growth factor beta (TGFβ) receptors are single pass serine/threonine kinase receptors. They exist in several different isoforms that can be homo- or heterodimeric.Three TGFβ superfamily receptors specific for TGFβ, the TGFβ receptors, can be distinguished by their structural and functional properties. TGFβR1 (ALK5) and TGFβR2 have similar ligand-binding affinities and can be distinguished from each other only by peptide mapping. Both TGFβR1 and TGFβR2 have a high affinity for TGFβ1 and low affinity for TGFβ2. TGFβR3 (β-glycan) has a high affinity for both homodimeric TGFβ1 and TGFβ2 and in addition the heterodimer TGF-β1.2. The TGFβ receptors also bind TGFβ3.
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SIS3是选择性 Smad3 抑制剂， 抑制 TGF-βR1信号通路。
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R 268712是TGF-βRI的活性选择性抑制剂。
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NG 25是TGF-β-activated kinase (TAK1) 抑制剂。
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Galunisertib是有效的TGFβ receptor I (TβRI)抑制剂，IC50为56 nM。
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SB431542是一种有效的，选择性的ALK5抑制剂，IC50为94 nM，对ALK5的作用比对p38，MAPK和其他激酶强100倍。
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