tgf-β-smad3

TGF-β1/Smad3-IN-1 (Compound 5aa) is an orally administrable dual inhibitor of TGF-β1/Smad3 with anti-fibrotic activity and can be used for the study of idiopathic pulmonary fibrosis (IPF).

Caerulomycin A (Caerulomycin) (Cerulomycin; Caerulomycin) is an antifungal compound. Which induces generation of T cells, enhances TGF-β-Smad3 protein signaling via suppressing interferon-γ-induced STAT1 signaling. Antifungal and antibiotic activity, and used in autoimmune diseases.

NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor that disrupts the [SIX1/EYA2] complex, EMT, and metastasis.

SIS3 free base is a potent and selective inhibitor of Smad3 phosphorylation, effectively inhibiting the TGF-β1-induced myofibroblast differentiation of fibroblasts.

(E)-SIS3 (SIS3) is a Smad3 inhibitor (IC50=3 μM) and is selective. (E)-SIS3 inhibits the differentiation of fibroblasts into myofibroblasts via 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 TGF-β-induced accumulation of total collagen in NRK-49F cells, with an IC50 value of 4.31 μM. It also suppresses the TGF-β-induced in vitro expression of COL1A1, α-SMA, and p-Smad3. Additionally, TGFβ-IN-2 shows promise as a potential anti-fibrosis compound for in vivo applications through oral administration [1].

Halofuginone (RU-19110), the competitive inhibitor of prolyl-tRNA synthetase(Ki=18.3 nM), could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in the mammal.

2-APQC is a selective, orally active Sirtuin-3 (SIRT3) agonist (Kd=2.756 μM) that modulates mitochondrial homeostasis. It attenuates ISO-induced myocardial hypertrophy and fibrosis in vivo and in vitro, making it suitable for heart failure research. 2-APQC inhibits mTOR-p70S6K, JNK, TGF-β/Smad3, and ROS-p38MAPK pathways while activating PYCR1 and AMPK-Parkin, thereby suppressing necrosis and mitigating mitochondrial oxidative damage.

Halofuginone (Standard) is the standard substance of Halofuginone, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Halofuginone (RU-19110), the competitive inhibitor of prolyl-tRNA synthetase(Ki=18.3 nM), could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in the mammal.

ETTAC-2 is an LRG1 PROTAC degrader that facilitates the ubiquitination and degradation of LRG1, with a DC50 of 8.38 µM. It inhibits the TGF-β-Smad3 signaling pathway and reduces the secretion of proteins associated with fibrosis. ETTAC-2 can slow the progression of renal fibrosis.

ETTAC-2 acetate is a selective PROTAC degrader targeting LRG1 (Leucine-rich α-2 glycoprotein 1), inhibiting the TGF-β-Smad3 signalling pathway to slow renal fibrosis progression.

Chebulinic acid is a potent inhibitor of M. tuberculosis DNA gyrase. It also can inhibit SMAD-3 phosphorylation and H+ K+-ATPase activity.