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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LY2109761是一种新型的，选择性的TGF-β receptor type I/II (TβRI/II)双重抑制剂，Ki分别为38 nM和300 nM，同时也抑制Smad2的磷酸化。
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SB525334是一种有效的，选择性的TGFβ receptor I (ALK5)抑制剂，IC50为14.3 nM，作用于ALK4比作用于ALK5效果低4倍，可抑制ALK2， 3，和6活性。
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SB505124是TGFβ受体ALK4和ALK5抑制剂，IC50分别为129 nM和47 nM，还能抑制ALK7，但对ALK1，2，3和6无抑制性。
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GW788388, 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。
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EW-7197是一种高效的，选择性的，口服生物有效的TGF-β receptor ALK4/ALK5抑制剂，IC50分别为13 nM 和 11 nM。
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