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-P0118B
    Disitertide diammonium
    Inhibitor 99.53%
    Disitertide (P144) diammonium is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide diammonium is also a PI3K inhibitor and an apoptosis inducer.
    Disitertide diammonium
  • 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 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-108527
    CD1530
    98.13%
    CD1530 is an orally active, selective RARγ agonist and antibacterial agent. CD1530 reduces Smad1/5/8 phosphorylation and overall Smad levels. CD1530 reduces β-catenin, MMP9 protein, and ROS levels. CD1530 exhibits activities such as inhibiting heterotopic ossification, promoting Achilles tendon healing, and inhibiting muscle fatty infiltration. CD1530 can be used in the research of orthopedic diseases (such as heterotopic ossification, Achilles tendon injury), muscle diseases (such as muscle fatty infiltration-related diseases).
    CD1530
  • HY-12953
    R-268712
    Inhibitor 99.88%
    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.
    R-268712
  • HY-W012977
    3,3-Dimethyl-1-butanol
    Inhibitor 99.56%
    3,3-Dimethyl-1-butanol (DMB) is an orally active inhibitor of trimethylamine (TMA) and trimethylamine N-oxide (TMAO). 3,3-Dimethyl-1-butanol inhibits the signaling pathway of p65 NF-κB and TGF-β1/Smad3. 3,3-Dimethyl-1-butanol has potential applications in cardiovascular disease (CVD).
    3,3-Dimethyl-1-butanol
  • HY-B0252
    Hydrochlorothiazide
    Inhibitor 99.51%
    Hydrochlorothiazide (HCTZ), an orally active diuretic agent 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.
    Hydrochlorothiazide
  • HY-P99388
    Trevogrumab
    Inhibitor 98.86%
    Trevogrumab (REGN-1033) is a monoclonal antibody targeting GDF8 (growth differentiation factor 8, also known as myostatin). Trevogrumab is used in research on muscle wasting conditions, including disuse atrophy, chronic diseases, and changes in food and nutrient intake.
    Trevogrumab
  • HY-150795
    SY-LB-35
    Inhibitor ≥98.0%
    SY-LB-35 is a potent bone morphogenetic protein (BMP) receptor agonist. SY-LB-35 can stimulate significant increases in cell number and cell viability in the C2C12 myoblast cell line, and causes shifts towards the S and G2/M phases of the cell cycle. SY-LB-35 stimulates canonical Smad and non-canonical PI3K/Akt, ERK, p38 and JNK intracellular signaling pathways.
    SY-LB-35
  • HY-N0847
    Micheliolide
    Inhibitor 99.84%
    Micheliolide is a sesquiterpene lactone with anti-cancer and anti-inflammatory effects, which is derived from Michelia compressa and Michelia champaca. Micheliolide can attenuate high glucose-stimulated NF-κB activation, IκBα degradation, and the expression of MCP-1, TGF-β1, and FN in mouse mesangial cells. Micheliolide inhibits LPS (HY-D1056)-induced activation of NF-κB and PI3K/Akt/p70S6K pathways to play an anti-inflammatory role. Micheliolide inhibits dextran sodium sulphate (DSS) (HY-116282)-induced inflammatory intestinal disease, colitis-associated cancer and rheumatic arthritis.
    Micheliolide
  • 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.
    Trimethylamine N-oxide dihydrate
  • HY-P99708
    Livmoniplimab
    Inhibitor 99.25%
    Livmoniplimab (ABBV-151) is a monoclonal antibody against GARP/TGF-β1 that can inhibit the release of active TGF-β1. Livmoniplimab has anti-tumor activity in colon cancer mice. Livmoniplimab can be used for the study of locally advanced or metastatic solid tumors.
    Livmoniplimab
  • HY-P99441
    Apitegromab
    Inhibitor 99.51%
    Apitegromab (SRK-015) is an anti-promyostatin monoclonal antibody. Apitegromab can be used for the research of neuromuscular disease including spinal muscular atrophy.
    Apitegromab
  • HY-N2033
    Chebulinic acid
    Inhibitor 99.68%
    Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.
    Chebulinic acid
  • HY-W011121
    2-Oleoylglycerol
    Activator ≥99.0%
    2-Oleoylglycerol (2-OG) is a lipid found in the diet. It is a GPR119 agonist, with an EC50 value of 2.5 μM in activating hGPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol enhances the inflammatory response of macrophages and promotes fibrosis by activating the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. It also stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. 2-Oleoylglycerol is expected to be used in the research of non-alcoholic steatohepatitis (NASH) .
    2-Oleoylglycerol
  • HY-P99370
    Landogrozumab
    Inhibitor 99.54%
    Landogrozumab (LY2495655) is an humanized anti-myostatin monoclonal antibody. Landogrozumab effectively improves muscle volume, hand grip strength and function. Landogrozumab can be used for the research of muscle wasting disease.
    Landogrozumab
  • HY-116084S
    Trimethylamine N-oxide-d9
    Activator 99.76%
    Trimethylamine N-oxide-d9 is the deuterium labeled Trimethylamine N-oxide. 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[1][2][3].
    Trimethylamine N-oxide-d<sub>9</sub>
  • HY-P99590A
    Sotatercept (mIgG2a)
    Inhibitor 99.71%
    Sotatercept (mIgG2a) has direct cardioprotective actions, which reduces right ventricular (RV) remodeling and improves function in a pulmonary artery banding (PAB) mouse model.
    Sotatercept (mIgG2a)
  • HY-P99494
    Carotuximab
    Inhibitor
    Carotuximab (TRC105) is a IgG1 monoclonal antibody that blocks endoglin (CD105) and its downstream Smad signaling pathway. Carotuximab has immunomodulatory and antineoplastic actions.
    Carotuximab
  • HY-P99518
    Taldefgrobep alfa
    Inhibitor 98.65%
    Taldefgrobep alfa (BMS 986089; RG 6206; RO 7239361) is a potent inhibitory antibody targeting to human myostatin. Taldefgrobep alfa is a fusion protein composed of a human IgG1-Fc domain and Adnectin domain. Taldefgrobep alfa can be used for spinal muscular atrophy (SMA) research.
    Taldefgrobep alfa
  • HY-N1499
    Nystose
    Activator 99.93%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity