smad-3

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.

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

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.

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).

R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor.

GED-0507-34 Levo ((S)-3-(4-Aminophenyl)-2-methoxypropanoic acid), an orally available PPARγ modulator for amelioration of inflammation-driven intestinal fibrosis, decreased the expression of the pro-fibrotic genes Acta2, COL1a1, and Fn1, reduced the protein levels of α-SMA and collagen I-II, the main markers of fibrosis, as well as the major components of the TGFβ/Smad pathway, and decreased the expression of IL-13, CTGF, TGFB and ACTA1, and inhibited TGF-β-induced activation of fibroblasts and IECs cell lines.

1. Decursin (Decursinol angelate) is able to attenuate kainic acid-induced seizures and could have potential as an antiepileptic drug. 2. Decursin exhibits hepatoprotective effects , potentially by inhibiting the TGF-β1 induced NOX activation and Smad signaling. 3. Decursin has anti-cancer activity , mediated suppression of the PKCα, MAPK and NF-κB pathways in MCF-7 cells. 4. Decursin exhibits cytotoxicity against various human cancer cells and to possess anti-amnesic activity in vivo through the inhibition of AChE activity.

BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).

TGFβRI-IN-3 is a highly selective TGFβR1 inhibitor with an IC50 of 0.79 nM and exhibits 2000-fold selectivity against MAP4K4, showing potential applications in immuno-oncology [1].

Chebulinic acid (Standard) is a reference standard for research and analysis in studies involving Chebulinic acid. Chebulinic acid is a potent inhibitor of M. tuberculosis DNA gyrase. It also can inhibit SMAD-3 phosphorylation and H+ K+-ATPase activity.

Isoangustone A is a natural product that inhibits PI3K, MKK4, and MKK7 through ATP competition, suppresses the expression of G1 phase regulatory proteins, inhibits the phosphorylation of Akt, GSK-3β, and JNK1/2, and inhibits the proliferation of human melanoma cells and tumour growth in xenograft mouse models.