TGF-β/Smad-IN-3 

TGF-β/Smad-IN-3 (Compound 4w) is an effective TGF-β/Smad inhibitor. TGF-β/Smad-IN-3 exerts anti-pulmonary fibrosis activity by simultaneously inhibiting the TGF-β/Smad and MAPK signaling pathways. TGF-β/Smad-IN-3 significantly inhibits collagen deposition induced by TGF-β1, with its IC₅₀ value being 3.21 μM. TGF-β/Smad-IN-3 has an IC₅₀ of 46.77 nM for the autocrine motility factor (ATX). TGF-β/Smad-IN-3 significantly reduces the expression levels of α-SMA, COL1A1 and FN in TGF-β1-induced CCC-HPF-1 cells, and effectively inhibited TGF-β1-induced cell migration. TGF-β/Smad-IN-3 can be used for the study of pulmonary fibrosis^[1].

697.85

C₃₈H₅₃F₂N₅O₅

3100351-69-4

O=C(C1=NN=C2CN(C(CC[C@H]([C@H]3CC[C@@]4([H])[C@]5([H])[C@@H](O)C[C@]6([H])C[C@H](O)CC[C@]6(C)[C@@]5([H])CC[C@]34C)C)=O)CCN21)NCC7=CC=CC(OC(F)F)=C7

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• [1]. Hu Y, et al. Design, synthesis and evaluation of novel UDCA-tetrahydropyrazine triazole hybrids for the treatment of pulmonary fibrosis. Bioorg Chem. 2025 Oct 3;166:109064.