1. Signaling Pathways
  2. Stem Cell/Wnt
    TGF-beta/Smad
  3. TGF-beta/Smad

TGF-beta/Smad

Transforming growth factor beta

Transforming growth factor-beta (TGF-β) is a member of a superfamily of pleiotropic proteins that regulate multiple cellular processes such as growth, development and differentiation. The intracellular effectors of TGF-beta signalling, the Smad proteins, are activated by receptors and translocate into the nucleus, where they regulate transcription. Although this pathway is inherently simple, combinatorial interactions in the heteromeric receptor and Smad complexes, receptor-interacting and Smad-interacting proteins, and cooperation with sequence-specific transcription factors allow substantial versatility and diversification of TGF-beta family responses. Other signalling pathways further regulate Smad activation and function.

In addition, TGF-beta receptors activate Smad-independent pathways that not only regulate Smad signalling, but also allow Smad-independent TGF-beta responses. Aberrant TGF-β signaling is associated with a variety of diseases, such as fibrosis, cardiovascular disease and cancer. Hence, the TGF-β signaling pathway is recognized as a potential drug target.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-162404
    Smad2/3-IN-2
    Inhibitor
    Smad2/3-IN-2 (Compound 3) is an inhibitor for TGF-β-dependent Smad2/3 and IL-4-dependent STAT6 signaling pathway, with IC50s of 90 and 20 nM, respectively.
    Smad2/3-IN-2
  • HY-N0587R
    Demethylzeylasteral (Standard)
    Inhibitor
    Demethylzeylasteral (Standard) is the analytical standard of Demethylzeylasteral. This product is intended for research and analytical applications. Demethylzeylasteral is an orally active triterpenoid compound isolated from Tripterygium wilfordii, which has functions such as anti-inflammatory, anti-tumor, anti fertility, estrogen metabolism regulation, immune suppression, and immune system regulation .
    Demethylzeylasteral (Standard)
  • HY-N10577
    Chlorfortunone A
    Inhibitor
    Chlorfortunone A is a novel sesquiterpenoid dimers, can be isolated from the roots of Chloranthus fortunei. Chlorfortunone A inhibits transforming growth factor (TGF)-β activity.
    Chlorfortunone A
  • HY-149136
    MORF-627
    Inhibitor
    MORF-627 is a selective, orally active inhibitor for integrin αvβ6 with an IC50 of 9.2 nM measuring by human serum ligand binding assay. MORF-627 inhibits αvβ6-mediated TGF-β1 activation with an IC50 of 2.63 nM, inhibits SMAD2/3 phosphorylation with an IC50 of 8.3 nM. MORF-627 ameliorates the Bleomycin (HY-108345)-induced mouse lung fibrosis.
    MORF-627
  • HY-159692A
    AZD8701 sodium
    Inhibitor
    AZD8701 (IONIS-1063734) sodium is an antisense oligonucleotide targeting FOXP3 in regulatory T cells (Tregs). AZD8701 sodium can relieve immunosuppression in cancer.
    AZD8701 sodium
  • HY-P990720
    Elritercept
    Inhibitor
    Elritercept (KER-050) is a recombinant fusion protein comprising a modified activin receptor type IIA extracellular domain fused to a human IgG1 Fc. Elritercept inhibits activin A and other select TGF-β superfamily ligands.
    Elritercept
  • HY-N6896R
    Isoviolanthin (Standard)
    Inhibitor
    Isoviolanthin (Standard) is the analytical standard of Isoviolanthin. This product is intended for research and analytical applications. Isoviolanthin, a flavonoid glycoside, could markedly inhibit TGF-β1-mediated migration and invasion by deactivating epithelial-mesenchymal transition (EMT) via the TGF-β/Smad and PI3K/Akt/mTOR pathways in HCC cells. Isoviolanthin exhibits no cytotoxic effects on normal liver LO2 cells.
    Isoviolanthin (Standard)
  • HY-162729
    LSD1-IN-34
    Inhibitor
    LSD1-IN-34 (Compound 7d) is the orally active inhibitor for Lysine-specific demethylase (LSD) and monoamine oxidase (MAO), with IC50 of 4.51 and 18.46 nM, for LSD1 and MAO A. LSD1-IN-34 inhibits the Ang II-induced neonatal rat myocardial fibroblasts (NRCFs) activation, without significant toxicity (20 μM). LSD1-IN-34 inhibits TGFβ/Smad signaling pathway, and ameliorates heart failure in mice. LSD1-IN-34 exhibits good pharmacokinetic characteristics in rats.
    LSD1-IN-34
  • HY-N8261
    Amicoumacin B
    Inducer
    Amicoumacin B can be produced by actinomycete, strain 04-5195T.. Amicoumacin B increases the expression of bone morphogenetic protein 2 (BMP-2). Amicoumacin B has inhibitory effect against C. violaceum (MIC = 250 µg/mL). Amicoumacin B has quorum sensing inhibitory activity, and reduces the expression of the C. violaceum operons vioA, vioB, vioD, and vioE, but increases the expression of vioC.
    Amicoumacin B
  • HY-155786
    3,7-DMF
    Inhibitor
    3,7-DMF is an orally active inhibitor of TGF-β1-induced activation of HSCs. 3,7-DMF induces antioxidant genes and quenches ROS away, which can be used to study liver fibrosis.
    3,7-DMF
  • HY-N0439R
    Asiaticoside (Standard)
    Modulator
    Asiaticoside (Standard) is the analytical standard of Asiaticoside. This product is intended for research and analytical applications. Asiaticoside, a trisaccaride triterpene from Centella asiatica, suppresses TGF-β/Smad signaling through inducing Smad7 and inhibiting TGF-βRI and TGF-βRII in keloid fibroblasts; Asiaticoside shows antioxidant, anti-inflammatory, and anti-ulcer properties.
    Asiaticoside (Standard)
  • HY-159692
    AZD8701
    Inhibitor
    AZD8701 (IONIS-1063734) is an antisense oligonucleotide targeting FOXP3 in regulatory T cells (Tregs). AZD8701 can relieve immunosuppression in cancer.
    AZD8701
  • HY-P3603
    a-TGF (34-43), rat
    a-TGF (34-43), rat is an active peptide. a-TGF (34-43), rat can be used in the research of immunity.
    a-TGF (34-43), rat
  • HY-N0158R
    Oxymatrine (Standard)
    Inhibitor
    Oxymatrine (Standard) is the analytical standard of Oxymatrine. This product is intended for research and analytical applications. Oxymatrine, an alkaloid from Sophora flavescens Alt. with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and TGF-β/Smad pathway. Oxymatrine inhibits bocavirus minute virus of canines (MVC) replication, reduces viral gene expression and decreases apoptosis induced by viral infection.
    Oxymatrine (Standard)
  • HY-P990733
    Cibotercept
    Inhibitor
    Cibotercept is an anti-MSTN/INHBA/GDF11 monoclonal antibody.
    Cibotercept
  • HY-116084S1
    Trimethylamine-N-oxide-13C3
    Activator
    Trimethylamine-N-oxide-13C3 is the 13C-labeled Trimethylamine N-oxide. Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway[1][2][3].
    Trimethylamine-N-oxide-<sup>13</sup>C<sub>3</sub>
  • HY-170540
    NOX4-IN-1
    Inhibitor
    NOX4-IN-1 (Compound 14m) is the inhibitor for NADPH oxidase 4 (NOX4), and blocks the generation of ROS. NOX4-IN-1 inhibits TGF-β1/Smad signaling pathway, decreases the expression of fibrosis-related proteins. NOX4-IN-1 inhibits the cell migration of NRK-49F.
    NOX4-IN-1
  • HY-N2033R
    Chebulinic acid (Standard)
    Inhibitor
    Chebulinic acid (Standard) is the analytical standard of Chebulinic acid. This product is intended for research and analytical applications. Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.
    Chebulinic acid (Standard)
  • HY-N1584BR
    Halofuginone (hydrochloride) (Standard)
    Inhibitor
    Halofuginone (hydrochloride) (Standard) is the analytical standard of Halofuginone (hydrochloride). This product is intended for research and analytical applications. Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects[4].
    Halofuginone (hydrochloride) (Standard)
  • HY-162405
    Smad2/3-IN-1
    Inhibitor
    Smad2/3-IN-2 (Compound 27) is an inhibitor for TGF-β-dependent Smad2/3 and IL-4-dependent STAT6 signaling pathway, with IC50s of 90 and 20 nM, respectively.
    Smad2/3-IN-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity