SMAD
SMADs are intracellular proteins that transduce extracellular signals from transforming growth factor beta ligands to the nucleus where they activate downstream gene transcription. The SMADs, which form a trimer of two receptor-regulated SMADs and one co-SMAD, act as transcription factors that regulate the expression of certain genes. Specifically, colocalization of phosphorylated Smad1/5/8 complex and DLX3 regulate role for BMP signaling to Dlx3 during hair morphogenesis in animal models.
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LY364947(HTS466284)是TGF(beta)R-I高效ATP竞争性抑制剂，IC50值为59nM，对TGF(beta)R-II的抑制活性弱7倍。
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RepSox是一种选择性TGFβ/ALK5抑制剂，抑制ATP与ALK5结合以及ALK5自磷酸化时， IC50分别为23 nM和4 nM。
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LDN-193189是一种选择性的BMP信号通路抑制剂，抑制BMP I型受体ALK2和ALK3的转录活性，IC50分别为5 nM和30 nM，作用于BMP比作用于TGF-β选择性高200倍。
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Pirfenidone抑制TGF-β产生和TGF-β刺激的胶原蛋白产生，且降低TNF-α和IL-1β产量，具有抗纤维化和抗炎特性。
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LDN193189 HCl是LDN193189的盐酸盐,这是一种选择性BMP信号抑制剂,它能抑制BMP type I receptors ALK2和ALK3的转录活性，其 IC50 为 5 nM 和 30 nM, 并且对于BMP的选择性是对TGF-β选择性的200倍。
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