tgf-β-smad3

Caerulomycin A (Caerulomycin) 是抗真菌和抗细菌化合物，能够诱导 T 细胞的产生。它能够抑制 IFN-γ 诱导的 STAT1 通路，从而增强 TGF-β-Smad3 信号通路。它可用于自身免疫病的研究。

(E)-SIS3 (SIS3) 是 Smad3 的选择性抑制剂，能够抑制 Smad3 磷酸化(IC50:3 μM)。它利用 TGF-β1 抑制成纤维细胞向肌成纤维细胞分化。

SIS3 free base is a potent and selective Smad3 phosphorylation inhibitor. SIS3 free base inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.

ALK5-IN-8 is a highly effective inhibitor of TGFβRI (ALK5). It hinders the phosphorylation of ALK5 on downstream signaling proteins (Smad2 or Smad3) by obstructing the interaction between TGFβRI and ligands. Consequently, it disrupts or prevents TGF-β signaling. ALK5-IN-8 shows promise in the study of diverse diseases associated with ALK5-mediated pathways[1].

TGFβ-IN-2 (Compound 9d) effectively inhibits the accumulation of total collagen induced by TGF-β in NRK-49F cells, with an IC 50 value of 4.31 μM. It also suppresses the in vitro protein expression of COL1A1, α-SMA, and p-Smad3, which are induced by TGF-β. Additionally, TGFβ-IN-2 shows promise as a potential anti-fibrosis compound for in vivo applications through oral administration [1].

Halofuginone (RU-19110) 是Febrifugine 的衍生物，是一种竞争性脯氨酰-tRNA 合成酶抑制剂。它也是肺血管扩张剂，可激活Kv 通道并阻断电压门控、受体操作和存储操作的钙离子通道。它具有抗炎、抗癌、抗疟疾和抗纤维化作用。

NCGC00378430 是一种 SIX1 EYA2 相互作用抑制剂。它部分逆转 SIX1 过表达介导的转录和代谢谱，并逆转 SIX1 诱导的 TGF-β 信号传导和上皮-间质转化。在小鼠模型中，它能够抑制 SIX1 介导的乳腺癌转移。

ETTAC-2 是一种LRG1PROTAC降解剂，能够促进LRG1的泛素化和降解 (DC50为8.38 µM)。它抑制TGF-β-Smad3信号通路，减少与纤维化相关的蛋白分泌，并能有效减缓肾纤维化的进展。

Chebulinic acid 是从诃子果中提取的一种天然产物，结核分枝杆菌 DNA 促旋酶的有效抑制剂。它也能抑制 SMAD-3 phosphorylation 和 H+ K+-ATPase 的活性。