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-N3674
    Dalbergioidin
    Inhibitor
    Dalbergioidin, a well-known anthocyanin, ameliorates doxorubicin-induced renal fibrosis by suppressing the TGF-β signal pathway. Dalbergioidin exhibits tyrosinase inhibitory activity with an IC50 of 20 mM.
    Dalbergioidin
  • HY-W109107
    GED 0507-34-Levo
    Inhibitor
    GED 0507-34-Levo is an orally active PPARγ modulator. GED 0507-34-Levo downregulates the expression of TGF-β, Smad3, IL-13, and CTGF in the colon. GED 0507-34-Levo improves DSS-induced chronic colitis and fibrosis.
    GED 0507-34-Levo
  • HY-162404
    (14S,15R)-14-Deoxyoxacyclododecindione
    Inhibitor
    (14S,15R)-14-Deoxyoxacyclododecindione (Compound 3) acts as an inhibitor of TGF-β-dependent Smad2/3 and IL-4-dependent STAT6, with IC50 values of 90 nM and 20 nM, respectively. (14S,15R)-14-deoxyoxacyclododecindione is a potent IL-4 inhibitor with an IC50
    value of 20 nM. (14S,15R)-14-Deoxyoxacyclododecindione is applicable to the research of chronic inflammation and fibrotic diseases.
    (14S,15R)-14-Deoxyoxacyclododecindione
  • HY-178328
    VDR agonist 4
    Inhibitor
    VDR agonist 4 is an orally active potent VDR agonist. VDR agonist 4 exerts VDR-dependent antifibrotic activity by regulating multiple fibrosis-related genes to suppress α-SMA and collagen I production, thereby inhibiting hepatic stellate cell (HSC) activation. VDR agonist 4 improves CCl4 (HY-RS16594)-induced hepatic fibrosis in mice. VDR agonist 4 can be used for liver fibrosis research.
    VDR agonist 4
  • 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-P11753
    IKVAVC
    Inhibitor
    IKVAVC is a derivative peptide of IKVAV with an artificially added cysteine (Cys) at its C-terminus. IKVAVC retains all the biological activities of the original IKVAV, mainly acting as a neural adhesion/differentiation signaling peptide, and is equipped with an engineered linker arm that enables covalent conjugation to molecular materials. IKVAV inhibits the migration and activation of fibroblasts, downregulates the TGF-β1 signaling pathway and endoplasmic reticulum stress, and promotes nerve repair. IKVAV regulates the phenotype of macrophages, shifting them from the pro-inflammatory M1 type to the pro-reparative M2 type.
    IKVAVC
  • HY-182795
    Colchicine derivative-1
    Inhibitor
    Colchicine derivative-1 is a colchicine derivative. Colchicine derivative-1 exhibits cytotoxicity against various cells. Colchicine derivative-1 arrests cancer cells at the G2/M phase of the cell cycle. Colchicine derivative-1 increases the levels of MMP-2, MMP-8, MMP-9, IL-2, IL-6, IL-17A, IL-22, IL-4, and IL-5 in the blood, inhibits the gene expression of hepatic fibrinogen α, β, γ and TGF-β1, and alleviates hepatic fibrosis symptoms in mice. Colchicine derivative-1 has antifibrotic activity and can be used in studies related to hepatic fibrosis.
    Colchicine derivative-1
  • HY-N6896R
    Isoviolanthin (Standard)
    Inhibitor
    Isoviolanthin (Standard) is the analytical standard of Isoviolanthin (HY-N6896). This product is intended for research and analytical applications. 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 (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-179042
    TGF-β/Smad-IN-3
    Inhibitor
    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.
    TGF-β/Smad-IN-3
  • HY-181430
    PXS 25
    Inhibitor
    PXS 25 is a cation-independent mannose 6-phosphate receptor (CI-M6PR) inhibitor that inhibits CI-M6PR-mediated activation of latent TGF-β1. PXS 25 inhibits conversion of high glucose-induced latent TGF-β1 to active TGF-β1 in proximal tubule cells under normoxic conditions. PXS 25 suppresses high glucose-induced fibronectin, collagen IV production, and phosphorylated Smad 2 in proximal tubule cells under normoxic conditions. PXS 25 has antifibrotic properties in skin fibroblasts. PXS 25 can be used for the research of diabetic nephropathy.
    PXS 25
  • HY-P992076
    Anti-Candida auris β-1, 3 glucans Antibody (2G8)
    Inhibitor
    Anti-Candida auris β-1,3-glucans Antibody (2G8) is an antibody targeting Candida auris β-1,3-glucans, and also acts as an inhibitor of AChE and TGF-β receptor 2. Anti-Candida auris β-1,3-glucans Antibody (2G8) also targets fungal cell wall components, effectively inhibits fungal growth and interferes with capsule formation, thereby significantly reducing the fungal load in mouse tissues. Anti-Candida auris β-1,3-glucans Antibody (2G8) not only blocks TGF-β receptor binding to inhibit the Smad signaling pathway, reduces fibroblast activation and collagen deposition, but also induces epithelial differentiation of tumor cells and reduces pancreatic tumor metastasis. Anti-Candida auris β-1,3-glucans Antibody (2G8) specifically binds to the conserved N-linked glycoepitope on AChE to inhibit its activity without interfering with BChE, and can be used in studies of cryptococcosis and related tumor mechanisms.The isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-Candida auris β-1, 3 glucans Antibody (2G8)
  • 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-N0559R
    Kirenol (Standard)
    Inhibitor
    Kirenol (Standard) is the analytical standard of Kirenol (HY-N0559). This product is intended for research and analytical applications. Kirenol is a diterpenoid compound, an orally active apoptosis inducer and signaling pathway regulator, with a Kd value of 5.47 μM against the target CK2. Kirenol promotes the cleavage of Bid into tBid, regulates the protein levels/phosphorylation of Bax, Bcl-2, p53 and p21, and induces caspase-independent apoptosis, S-phase cell cycle arrest, ROS accumulation and cytotoxicity in cancer cells. Kirenol activates the CK2/AKT and AMPK-mTOR-ULK1 pathways, inhibits the signaling of NF-κB, TGF-β/Smads and NLRP3 inflammasome, and regulates the GSK3β, BMP and Wnt/β-catenin pathways. Kirenol induces autophagy, mitophagy and osteoblast differentiation, promotes mitochondrial fusion, and exerts antioxidant, anti-inflammatory, antifibrotic, renoprotective, cardioprotective, neuroprotective and analgesic effects. Kirenol is applicable to research related to chronic myeloid leukemia, ischemic stroke, diabetic nephropathy, heart failure, acute lung injury and osteoporosis.
    Kirenol (Standard)
  • HY-175662
    TGF-β/Smad-IN-2
    Inhibitor
    TGF-β/Smad-IN-2 is an orally active TGF-β/Smad inhibitor. TGF-β/Smad-IN-2 inhibits TGF-β-induced fibroblast-to-myofibroblast differentiation and collagen deposition, with an IC50 value of 102 μM for collagen reduction in LL29 cells. TGF-β/Smad-IN-2 exerts its effects through modulation of the SMAD3/SMAD7 signaling pathway. TGF-β/Smad-IN-2 reduces lung index in pulmonary fibrosis mice. TGF-β/Smad-IN-2 can be used for the study of pulmonary fibrosis.
    TGF-β/Smad-IN-2
  • HY-N16980
    (7'E,8S)-2',4,8-Trihydroxy-3-methoxy-2,4'-epoxy-8,5'-neolign-7'-en-7-one
    Inhibitor
    (7'E,8S)-2',4,8-Trihydroxy-3-methoxy-2,4'-epoxy-8,5'-neolign-7'-en-7-one (compound 4) is a novel neolignan anti-inflammatory agent. (7'E,8S)-2',4,8-Trihydroxy-3-methoxy-2,4'-epoxy-8,5'-neolign-7'-en-7-one has an IC50 of 25.2 μM against TGF-β-induced hepatic stellate cells (HSC-T6). (7'E,8S)-2',4,8-Trihydroxy-3-methoxy-2,4'-epoxy-8,5'-neolign-7'-en-7-one may be related to blocking excessive cell proliferation in the process of liver fibrosis and can be used in the study of liver fibrosis-related diseases. (7'E,8S)-2',4,8-Trihydroxy-3-methoxy-2,4'-epoxy-8,5'-neolign-7'-en-7-one can be naturally extracted from the dried aerial parts of Penthorum chinense Pursh.
    (7'E,8S)-2',4,8-Trihydroxy-3-methoxy-2,4'-epoxy-8,5'-neolign-7'-en-7-one
  • HY-17661
    Depiperazine-DM3189
    Inhibitor
    Depiperazine-DM3189 is a derivative of LDN193189 (HY-12071). LDN193189 is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.
    Depiperazine-DM3189
  • HY-100113A
    Buloxibutid hydrochloride
    Inhibitor
    Buloxibutid (AT2 receptor agonist C21) hydrochloride is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a Ki value of 0.4 nM for porcine AT2R. Buloxibutid hydrochloride exerts vasodilatory, anti-inflammatory, antifibrotic (promoting the expression of collagenase MMP-13) and tissue repair effects mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway and inflammatory NF-κB pathway. Buloxibutid hydrochloride can be used in research related to idiopathic pulmonary fibrosis, hypertension, systemic sclerosis and other conditions.
    Buloxibutid hydrochloride
  • HY-175205
    TGF-β2-IN-1
    Inhibitor
    TGF-β2-IN-1 is a selective TGF-β2 inhibitor. TGF-β2-IN-1 exhibits potent antiproliferative effects on HCT-116, Caco-2 and HT-29 with IC50 values of 6.84, 10.21, and 9.47 μM, respectively. TGF-β2-IN-1 inhibits TGF-β2 signaling in a dose-dependent manner by suppressing both receptor and cytokine expression.TGF-β2-IN-1 can be used for the study of colorectal cancer.
    TGF-β2-IN-1
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity