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

TGF-beta/Smad

Transforming growth factor beta

TGF-beta/Smad

Related Products

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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-158821
    ISTH0036
    		Inhibitor
    ISTH0036 is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 suppresses TGF-β2 expression, reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-to-mesenchymal transition, and inhibits angiogenesis while promoting bleb survival. ISTH0036 exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases.
    ISTH0036
  • HY-N1584B
    Halofuginone hydrochloride
    		Inhibitor
    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.
    Halofuginone hydrochloride
  • HY-W108953
    Myristoyl tetrapeptide-12
    		Activator
    Myristoyl tetrapeptide-12 directly activates SMAD2 and induces the linking of SMAD3 with DNA. Myristoyl tetrapeptide-12 is capable of stimulating hair growth, especially at the level of eyelashes.
    Myristoyl tetrapeptide-12
  • HY-Y1269D
    Ammonium chloride, for molecular biology
    		Inhibitor
    Ammonium chloride (Salmiac), for molecular biology is an inhibitor of Slc26a4 and SMAD2. Ammonium chloride, for molecular biology reduces the protein expression level of Slc26a4 in lung tissue, and attenuates ozone-induced increases in proinflammatory cytokines, inflammatory cells, pulmonary resistance, goblet cell hyperplasia, peribronchial inflammation and thiocyanate levels in mouse tissues and bronchoalveolar lavage fluid. Ammonium chloride, for molecular biology decreases the level of phosphorylated SMAD2, inhibits autophagy by reducing autophagy-related proteins, and enhances Cisplatin (HY-17394)-induced cancer cell apoptosis and DNA double-strand breaks. Ammonium chloride, for molecular biology also inhibits the TCA cycle, reduces ATP production, increases glucose utilization, regulates the levels of lactic acid, glutamic acid and ATP, and induces morphological degeneration of neuroblastoma cells. Ammonium chloride, for molecular biology can be used in studies related to ozone-induced airway injury, hepatocellular carcinoma, human cervical cancer, hepatic encephalopathy, Reye syndrome, epilepsy and neurodegenerative diseases.
    Ammonium chloride, for molecular biology
  • HY-168607
    ALK5-IN-83
    		Inhibitor
    ALK5-IN-83 (compound 13b) is a ALK5 inhibitor with the IC50 of 0.13 μM. ALK5-IN-83 inhibits TGF-β1-induced Smad2 phosphorylation and cell motility in A549 cells.
    ALK5-IN-83
  • 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-160215A
    GFH018 methylbenzenesulfonate
    		Modulator
    GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC50 of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma.
    GFH018 methylbenzenesulfonate
  • 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)
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Cat. No. Product Name / Synonyms Application Reactivity