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-B0673
    Pirfenidone
    		Inhibitor 99.99%
    Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities.
    Pirfenidone
  • HY-13013
    SIS3
    		Inhibitor 99.62%
    SIS3 is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation. SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.
    SIS3
  • HY-N1584
    Halofuginone
    		Inhibitor 99.28%
    Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
    Halofuginone
  • HY-100347
    SRI-011381
    		Agonist 99.58%
    SRI-011381 is an orally active TGF-β signaling agonist, exhibits neuroprotective effects.
    SRI-011381
  • HY-P99241
    Ponsegromab
    		Inhibitor 99.60%
    Ponsegromab is a Growth differentiation factor 15 (GDF15) inhibitor with human, cynomolgus monkey, and mouse target IC50 values of 0.123 nM, 0.053 nM, and 0.102 nM, respectively. Ponsegromab acts as a chemosensitizer, increases intracellular reactive oxygen species, reduces glutathione levels. Ponsegromab can be used for the research of oxaliplatin-resistant colorectal cancer.
    Ponsegromab
  • HY-142118C
    Trabedersen sodium scrambled negative control
    		Inhibitor
    Trabedersen sodium scrambled negative control is the sequence scrambled negative control of Trabedersen sodium.
    Trabedersen sodium scrambled negative control
  • HY-P11609
    TGFβ1-IN-4
    		Inhibitor
    TGFβ1-IN-4 is a TGF-β1 inhibitor. TGFβ1-IN-4 inhibits myofibroblast activation and epithelial-mesenchymal transition in vitro. TGFβ1-IN-4 alleviates renal fibrosis in a mouse model of renal fibrosis. TGFβ1-IN-4 can be used for research on fibrotic diseases such as renal fibrosis.
    TGFβ1-IN-4
  • HY-183067A
    TAS1440 benzoate
    		Activator
    TAS1440 benzoate is an orally active LSD1/KDM1A inhibitor with a human IC50 of 4.8 nM. TAS1440 benzoate non-covalently binds to the histone H3-binding pocket of LSD1, inhibiting demethylase activity and disrupting repressive complexes with INSM1 and SMAD2. TAS1440 benzoate activates tumor-suppressive TGF-β and NOTCH signaling pathways via transcriptional reprogramming. TAS1440 benzoate can be used for the research of small cell lung cancer, specifically the SCLC-A subtype.
    TAS1440 benzoate
  • HY-N0439
    Asiaticoside
    		Modulator 99.67%
    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
  • HY-16268
    Kartogenin
    		Activator 99.05%
    Kartogenin (KGN) is an inducer of chondrogenic tissue formation (EC50: 100 nM). Kartogenin induces chondrogenesis by binding to fibrin A, disrupting its interaction with the transcription factor core binding factor beta subunit (CBFβ), and by modulating the CBFβ-RUNX1 transcriptional program. Kartogenin also promotes tendon-bone junction (TBJ) wound healing by stimulating collagen synthesis. Kartogenin is widely used in cell-free therapy in the field of regeneration for cartilage regeneration and protection, tendon-bone healing, wound healing and limb development. Kartogenin promotes cartilage repair, coordinates limb development, and is also used in osteoarthritis (OA) research.
    Kartogenin
  • HY-116084
    Trimethylamine N-oxide
    		Activator 98.0%
    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.
    Trimethylamine N-oxide
  • HY-100347A
    SRI-011381 hydrochloride
    		Agonist 99.94%
    SRI-011381 hydrochloride is an orally active TGF-β signaling agonist, exhibits neuroprotective effects, with blood-brain barrier permeability.
    SRI-011381 hydrochloride
  • HY-W016562
    Hippuric acid
    		Activator 99.98%
    Hippuric Acid is an orally active metabolite. Hippuric Acid can be produced by intestinal microorganisms from the metabolism of polyphenols, benzoic acid. Hippuric Acid decreases NRF2, MMP9 and leads to ROS accumulation. Hippuric Acid activates TGFβ/SMAD signaling. Hippuric Acid improves hyperuricemia and colitis. Hippuric Acid can also be used in cardiovascular disease research. .
    Hippuric acid
  • HY-N0158
    Oxymatrine
    		Inhibitor 99.92%
    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
  • HY-112499
    Menaquinone-7
    		Activator 98.51%
    Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs (orally active), is originally discovered as the anti-hemorrhagic factors. Menaquinone-7 inhibits osteoclast bone resorption in vitro and stimulates bone formation in femoral tissue of aged female rats. Menaquinone-7 has a well-researched potential in the prevention of aging-induced bone degeneration. Menaquinone-7 is also a pharmacological option for activating Gla matrix protein and intervening in the progression of calcific aortic stenosis (CAVS).
    Menaquinone-7
  • HY-160623
    Rentosertib
    		Inhibitor 99.96%
    Rentosertib (INS018 055) (compound 112) is the orally active TNIK and MAP4K4 inhibitor with IC50 values of 12-120, 12-120 nM, respectively.
    Rentosertib
  • HY-P99020
    Fresolimumab
    		Inhibitor 99.51%
    Fresolimumab (GC1008) is a human monoclonal antibody against TGF-β that neutralizes all mammalian active subtypes of TGF-β. The binding affinity of Fresolimumab to TGF-β2 is 1.8 nM. Fresolimumab improves Bleomycin (HY-108345)-induced acute lung injury. Fresolimumab radiolabeled with 89Zr can be used for PET analysis of TGF-β expression, antibody uptake and organ distribution. Fresolimumab can be used in the study of cancer, osteogenesis imperfecta, fibrosis and kidney disease.
    Fresolimumab
  • HY-P99720
    Luspatercept
    		Inhibitor 98.92%
    Luspatercept (ACE-536) is a recombinant modified ActRIIB fusion protein that binds with transforming growth factor β superfamily ligands. Luspatercept increases the erythrocyte numbers and promotes maturation of erythroid precursors. Luspatercept binds with GDF11 and inhibits Smad2/3 signaling. Luspatercept can be used for the research of anemia.
    Luspatercept
  • HY-100113
    Buloxibutid
    		Inhibitor 98.94%
    Buloxibutid (AT2 receptor agonist C21) is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a Ki value of 0.4 nM for porcine AT2R. Buloxibutid exerts effects such as vasodilation, anti-inflammation, anti-fibrosis (promoting the expression of collagenase MMP-13) and tissue repair mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway as well as the inflammatory NF-κB pathway. Buloxibutid can be used in research related to idiopathic pulmonary fibrosis, hypertension, and systemic sclerosis.
    Buloxibutid
  • HY-N0587
    Demethylzeylasteral
    		Inhibitor 99.92%
    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 [1][2].
    Demethylzeylasteral
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity