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-124674A
    CCT365623 hydrochloride
    Activator 98.07%
    CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC50 of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties.
    CCT365623 hydrochloride
  • HY-P10634
    P17 Peptide
    98.30%
    P17 Peptide is a human TGF-β1 inhibitory peptide. P17 Peptide can block woodchuck TGF-β1 activity.
    P17 Peptide
  • HY-114683
    KS370G
    Inhibitor 99.71%
    KS370G is an orally active hypoglycemic and cardiovascular protective agent. KS370G improves left ventricular hypertrophy and function in pressure-overload mice heart. KS370G reduces renal obstructive nephropathy.
    KS370G
  • HY-N6896
    Isoviolanthin
    Inhibitor 99.87%
    Isoviolanthin is a flavonoid glycoside. Isoviolanthin can be extracted from Dendrobium officinale. Isoviolanthin has a strong affinity for binding to KDM6B, CHAC2, ESCO2, and IPO4. Isoviolanthin decreases MMP-2 and MMP-9. Isoviolanthin inhibits TGF-β/Smad and PI3K/Akt/mTOR signaling pathways. Isoviolanthin increases Fhl3 expression. Isoviolanthin has cytoprotective effects. Isoviolanthin has anticancer activity against hepatocellular carcinoma.
    Isoviolanthin
  • HY-100830A
    NCB-0970
    Control 98.81%
    NCB-0970 is the negative control of NCB-0846 (HY-100830). NCB-0846 is an orally active, selective inhibitor for Wnt, that inhibits Traf2- and Nck-interacting kinase (TNIK) with an IC50 of 21 nM. NCB-0846 blocks TGF-β signaling pathway by inhibiting SMAD2/3 phosphorylation and nuclear translocation.
    NCB-0970
  • HY-W005379
    DGM
    Inhibitor 99.99%
    DGM is an inhibitor of the TGF-β1/Smad signaling pathway with significant antifibrotic effects. DGM inhibits the epithelial-mesenchymal transition (EMT) process in alveolar epithelial cells and slows the progression of pulmonary fibrosis in vivo by reducing lung inflammation, improving lung function, and decreasing extracellular matrix (ECM) remodeling. DGM can be used in research on idiopathic pulmonary fibrosis (IPF) and EMT-related diseases.
    DGM
  • HY-159692
    AZD8701
    Inhibitor
    AZD8701 (IONIS-1063734) is an antisense oligonucleotide targeting FOXP3 in regulatory T cells (Tregs), with a human IC50 of 65.2 nM. AZD8701 binds to intronic sites of all FOXP3 pre-mRNA isoforms and mediates dose-dependent FOXP3 knockdown via free uptake. AZD8701 can be used in cancer-related research.
    AZD8701
  • HY-149136
    MORF-627
    Inhibitor
    MORF-627 is a highly selective, orally active integrin αvβ6 inhibitor. By blocking TGF-β1 activation and pSMAD2 signaling, MORF-627 significantly reduces collagen deposition, epithelial-mesenchymal transition markers, and structural changes in fibrotic cells. MORF-627 exhibits significant antifibrotic efficacy without genotoxicity in idiopathic pulmonary fibrosis models. However, MORF-627 induces bladder epithelial proliferation and early invasive urothelial carcinoma in cynomolgus monkeys and human cells, and this toxic effect can be reversed by exogenous TGF-β. MORF-627 can be used for studying the pathological mechanisms of pulmonary fibrosis and evaluating drug safety.
    MORF-627
  • HY-171878
    BI-4659
    Inhibitor 99.78%
    BI-4659 is a TGFβRI and PDGFRα inhibitor with IC50 values of 19 nM and 99 nM, respectively. BI-4659 inhibits the kinase activities of TGFβRI and PDGFRα, blocks the downstream TGFβRI signaling pathway, and reduces the phosphorylation level of Smad2/3 without altering the expression of TGF-β1. BI-4659 is applicable to research related to pulmonary fibrosis, cancer, and renal ischemia-reperfusion injury.
    BI-4659
  • HY-155786
    3,7-DMF
    Inhibitor 99.79%
    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-151289
    ALK5-IN-34
    Inhibitor 98.21%
    ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer.
    ALK5-IN-34
  • HY-169004
    CBT-295
    Inhibitor 99.34%
    CBT-295 is an orally active autotaxin (ATX) inhibitor. CBT-295 exhibits a significant reduction in inflammatory cytokines like TGF-β, TNF-α and IL-6 levels, also reduced bile duct proliferation marker CK-19 and lowered liver fibrosis. The reversal of liver fibrosis with CBT-295 led to a reduction in blood and brain ammonia levels. CBT-295 also reduced neuroinflammation induced by ammonia. CBT-295 is promising for research of liver cirrhosis and associated encephalopathy.
    CBT-295
  • HY-N0168AS1
    (Rac)-Hesperetin-13C,d3
    Inhibitor 99.3%
    (Rac)-Hesperetin-13C,d3 is the 13C- and deuterium labeled (Rac)-Hesperetin. (Rac)-Hesperetin is the racemate of Hesperetin (HY-N0168), an orally active multi-target inhibitor. (Rac)-Hesperetin exhibits significant anti-tumor and anti-inflammatory activities by blocking the TGF-β1-mediated Fyn/RhoA signaling axis and the TLR4-MyD88-NF-κB inflammatory pathway. (Rac)-Hesperetin inhibits the formation of actin stress fibers and the migration and invasion of cancer cells, and is suitable for triple-negative breast cancer research. In inflammation models, (Rac)-Hesperetin effectively alleviates lung injury by reducing the release of pro-inflammatory mediators and regulating the activity of oxidative stress enzymes, and is suitable for acute lung injury research. (Rac)-Hesperetin also interferes with the entry and early replication processes of channel catfish virus, inhibits viral gene expression and progeny virus production, thereby protecting cells from virus-induced cytopathic effects.
    (Rac)-Hesperetin-<sup>13</sup>C,d<sub>3</sub>
  • HY-P99606
    Cirevetmab
    Inhibitor ≥99.0%
    Cirevetmab (ZTS-00521426) is an immunoglobulin G2-kappa, Canis lupus familiaris TGFB1 caninized monoclonal antibody. Cirevetmab is an immunomodulator.
    Cirevetmab
  • 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-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-N8261
    Amicoumacin B
    Inducer 98.8%
    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-P99695
    Lerdelimumab
    Inhibitor
    Lerdelimumab (CAT-152) is an IgG4 human anti-TGF-β2 recombinant monoclonal antibody. Lerdelimumab can be used as an anti-scarring agent for glaucoma research.
    Lerdelimumab
  • HY-N1499R
    Nystose (Standard)
    Activator
    Nystose (Standard) is the analytical standard of Nystose. This product is intended for research and analytical applications. Nystose is a tetrasaccharide with two fructose molecules linked via beta (1→2) bonds to the fructosyl moiety of sucrose. Nystose exhibits prebiotic, immunomodulatory, and metabolism regulating activities. Nystose promotes the bone mineralization by activating the Wnt/β-catenin signaling pathway.
    Nystose (Standard)
  • HY-117511
    HJC0123
    Inhibitor 99.06%
    HJC0123 is a STAT3 inhibitor. HJC0123 inhibits the proliferation of hepatic stellate cells and induces cell cycle arrest and apoptosis. HJC0123 reduces the phosphorylation, nuclear translocation and transcriptional activities of STAT3, increases the production of IL-6, inhibits the phosphorylation of Smad2/3 and down-regulates SOCS3. HJC0123 can be used in the study of liver fibrosis.
    HJC0123
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity