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
  • HY-B0673
    Pirfenidone
    Inhibitor 99.95%
    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.
  • HY-13013
    (E)-SIS3
    Inhibitor 98.02%
    (E)-SIS3 is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation. (E)-SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.
  • HY-16268
    Kartogenin
    Activator 98.30%
    Kartogenin (KGN) is an inducer of differentiation of human mesenchymal stem cells into chondrocytes, with an EC50 of 100 nM. Kartogenin binds filamin A, disrupts its interaction with the transcription factor core-binding factor β subunit (CBFβ), and induces chondrogenesis by regulating the CBFβ-RUNX1 transcriptional program. Kartogenin can be used for the research of osteoarthritis (OA).
  • HY-N0439
    Asiaticoside
    Modulator 99.84%
    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.
  • HY-100347A
    SRI-011381 hydrochloride
    Agonist 99.97%
    SRI-011381 hydrochloride is an orally active TGF-β signaling agonist, exhibits neuroprotective effects.
  • HY-P99241
    Ponsegromab
    Inhibitor
    Ponsegromab (PF 06946860) is a potent and selective humanized anti-GDF15 antibody inhibitor with anti-cachexia activity. Ponsegromab binds to GDF15 and prevents the binding of GDF15 to GFRAL, thereby blocking GDF15/GFRAL-mediated signaling. Ponsegromab can be used in the research of cancers.
  • HY-147025
    (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
    Inhibitor 99.06%
    (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine has a multi-path anti-fibrosis function and a renal protection function for research of renal anemia.
  • HY-151289
    ALK5-IN-34
    Inhibitor
    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.
  • HY-N1584
    Halofuginone
    Inhibitor 99.78%
    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.
  • HY-N0158
    Oxymatrine
    Inhibitor ≥98.0%
    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.
  • 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.
  • HY-B0252
    Hydrochlorothiazide
    Inhibitor 99.49%
    Hydrochlorothiazide (HCTZ), an orally active diuretic drug of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.
  • HY-N1584A
    Halofuginone hydrobromide
    Inhibitor 99.55%
    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.
  • HY-101275
    EMT inhibitor-1
    Inhibitor 99.27%
    EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.
  • HY-N0038
    Alantolactone
    Activator 99.94%
    Alantolactone is a selective STAT3 inhibitor, with potent anticancer activity. Alantolactone induces apoptosis in cancer.
  • HY-100347
    SRI-011381
    Agonist 99.58%
    SRI-011381 is an orally active TGF-β signaling agonist, exhibits neuroprotective effects.
  • HY-P0118A
    Disitertide TFA
    Inhibitor
    Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide TFA is also a PI3K inhibitor and an apoptosis inducer.
  • HY-12953
    R-268712
    Inhibitor 99.78%
    R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer.
  • HY-124674A
    CCT365623 hydrochloride
    Activator 98.11%
    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.
  • HY-108915
    Trimethylamine N-oxide dihydrate
    Activator ≥98.0%
    Trimethylamine N-oxide dihydrate is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide dihydrate induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide dihydrate also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.
Cat. No. Product Name / Synonyms Species Source