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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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。
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LDN-212854 是一种强效的选择性 BMP receptor 抑制剂， 其作用于ALK2的 IC50 为 1.3 nM , 分别超过作用于ALK1, ALK3, ALK4, 和 ALK5的选择性约 2-, 66-, 1641-, 和 7135倍。
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