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-P99857
    Domagrozumab
    Inhibitor
    Domagrozumab is an anti-myostatin humanized monoclonal antibody with a KD value of 2.6 pM for human myostatin. Domagrozumab induces muscle anabolic activity. Domagrozumab can be used in research of duchenne muscular dystrophy (DMD).
    Domagrozumab
  • HY-142118A
    Trabedersen sodium
    Inhibitor 98.81%
    Trabedersen (AP 12009) sodium is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen sodium blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen sodium exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen sodium is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma.
    Trabedersen sodium
  • HY-N7675
    Flavanomarein
    Inhibitor 99.92%
    Flavanomarein is a substance with cytoprotective, anti-inflammatory and antioxidant activities, with a Ka of 3.064e-5 M against human Syk. Flavanomarein enhances the phosphorylation level of AKT, regulates the expression of PKC-δ, P85α, PKC-β1, Sirt1, Bcl-2 and ICAD, and inhibits the nuclear translocation of NF-κB p65. Flavanomarein regulates EMT marker proteins, promotes the proliferation of HK-2 cells, and protects neuronal cells from 6-OHDA-induced neurotoxic damage. Flavanomarein can be used in studies related to Parkinson's disease and diabetic nephropathy.
    Flavanomarein
  • HY-P99359
    Elezanumab
    Inhibitor 99.91%
    Elezanumab (ABT-555; AE12-1Y-QL) is a human monoclonal antibody that selectively targets repulsive guidance molecule A (RGMa). Elezanumab potently inhibited RGMa mediated BMP signalling via the SMAD1/5/8 pathway, with an IC50 around 97 pM. Elezanumab promotes neuroregeneration and neuroprotection in neuronal injury and demyelination models binds N-terminal RGMa, blocks BMP signaling and lacks RGMc cross-reactivity. elezanumab has neuroregenerative and neuroprotective activities without impact on iron metabolism.
    Elezanumab
  • HY-119575
    Tetramethyluric acid
    Activator 99.63%
    Tetramethyluric acid (1,3,7,9-Tetramethyluric acid) is an orally active purine alkaloid in Coffea species and Camellia kucha. Tetramethyluric acid exhibits antiviral, and anti-inflammatory activity. Tetramethyluric acid can be used for the research of inflammation disease, and influenza virus infection.
    Tetramethyluric acid
  • HY-100448A
    Butaprost
    Inhibitor 99.85%
    Butaprost is a selective prostaglandin E receptor (EP2) agonist with an EC50 of 33 nM and a Ki of 2.4 μM for murine EP2 receptor. Butaprost is less activity against murine EP1, EP3 and EP4 receptors. Butaprost attenuates fibrosis by hampering TGF-β/Smad2 signalling.
    Butaprost
  • HY-W006957
    N6-(2-Hydroxyethyl)adenosine
    Inhibitor 99.85%
    N6-(2-Hydroxyethyl)adenosine is a purine nucleoside analog. N6-(2-Hydroxyethyl)adenosine inhibits NF-κB/Smad signaling pathway, exhibits anti-hyperglycemia, antioxidant, antitumor and anti-inflammatory and insecticidal activities. N6-(2-Hydroxyethyl)adenosine is orally active.
    N6-(2-Hydroxyethyl)adenosine
  • HY-P10899
    ETTAC-2
    Inhibitor 99.94%
    ETTAC-2 is a LRG1 PROTAC degrader, degrading LRG1 via the ubiquitin-proteasome pathway with a DC50 value of 8.38 μM. ETTAC-2 penetrates damaged renal cells to reduce the extracellular secretion of LRG1. ETTAC-2 effectively inhibits the TGF-β-Smad3 signaling pathway and diminishes the secretion of fibrosis-associated extracellular matrix proteins. ETTAC-2 degrades LRG1 within fibrotic kidneys and the efficacy in inhibiting the TGF-β-Smad3 pathway both in vitro and vivo. ETTAC-2 can be used for renal fibrosis research.
    ETTAC-2
  • HY-147372
    SJ000063181
    Activator 98.92%
    SJ000063181 is a potent BMP signaling activator. SJ000063181 activates BMP4 and the phosphorylation of SMAD1/5/8 (p-SMAD1/5/8). SJ000063181 induces ventralization in zebrafish embryos.
    SJ000063181
  • HY-N3266
    Methyl rosmarinate
    Inhibitor 99.89%
    Methyl rosmarinate is an orally active hydroxycinnamic acid. Methyl rosmarinate exhibits an IC50 of 24.70 μM and a Ki of 15.29 μM against PTP1B, an IC50 of 41.46 μg/mL against BChE, a Ki of 0.61 mM against mushroom tyrosinase, and an IC50 of 2.50 μM against SARS-CoV-2 3CLpro. Methyl rosmarinate downregulates the phosphorylation levels of ERK, JNK, p38, Smad2 and Smad3. Methyl rosmarinate activates erythrocyte BPGM and promotes the production of 2,3-BPG. Methyl rosmarinate induces apoptosis of fibroblasts. Methyl rosmarinate prolongs the survival time of hypoxic mice. Methyl rosmarinate improves insulin sensitivity. Methyl rosmarinate binds to SARS-CoV-2 3CLpro and inhibits viral replication. Methyl rosmarinate induces glioblastoma cell death. Methyl rosmarinate activates the TGR5/AMPK axis and reduces the levels of ROS and MDA. Methyl rosmarinate shows inhibitory activity against MMP-1. Methyl rosmarinate can be used in research related to pulmonary fibrosis, hypoxia-induced injury, type 2 diabetes, Alzheimer's disease, hyperpigmentation disorders, COVID-19, glioblastoma and myocardial ischemia-reperfusion injury.
    Methyl rosmarinate
  • HY-P5832
    BMP2-derived peptide
    Activator 98.04%
    BMP2-derived peptide is an osteogenic inducer and BMP receptor ligand. BMP2-derived peptide binds to BMP receptors on the cell surface to form a complex, activates the downstream Smad signaling pathway, and regulates the expression of osteogenic transcription factors. BMP2-derived peptide effectively promotes the adhesion, proliferation, osteogenic differentiation and mineralization of bone marrow mesenchymal stem cells, significantly up-regulates the mRNA levels of OCN, Runx2 and type I collagen, and increases alkaline phosphatase activity and calcium deposition. BMP2-derived peptide induces osteoblast differentiation and ectopic bone regeneration, and improves cranial bone defect repair. Meanwhile, BMP2-derived peptide enhances the cytocompatibility of mesoporous silica nanoparticles, synergistically increases osteogenic activity with Dexamethasone (HY-14648), serving as an important tool for bone defect repair research.
    BMP2-derived peptide
  • HY-P99518
    Taldefgrobep alfa
    Inhibitor 98.65%
    Taldefgrobep alfa (BMS 986089; RG 6206; RO 7239361) is a protein that blocks 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-P990667
    STX-100
    Inhibitor 99.99%
    STX-100 (BG00011) is a humanized monoclonal antibody targeting αVβ6 integrin. STX-100 specifically binds αVβ6 integrin, blocks latent TGF-β activation via latency-associated peptide (LAP) interaction prevention, and reduces profibrotic responses. STX-100 can be used for the research of idiopathic pulmonary fibrosis, and cancer.
    STX-100
  • HY-N2156
    Paeonolide
    99.58%
    Paeonolide, found in Paeonia suffruticosa, is an ERK1/2 activator. Paeonolide promotes early and late osteoblast differentiation, stimulates pre-osteoblast transmigration, and activates the BMP-Smad1/5/8, Wnt-β-catenin, JNK and p38 pathways. Paeonolide can be used for the research of osteoporosis, periodontitis.
    Paeonolide
  • HY-148234
    M4K2234
    Inhibitor 98.31%
    M4K2234, a chemical probe, is an orally active, highly selective inhibitor of ALK1 and ALK2 with IC50 values of 7 nM and 14 nM, respectively. M4K2234 specifically blocks BMP signaling by inhibiting the phosphorylation of SMAD1/5/8. M4K2234 inhibits BMP7-stimulated reporter gene activity (IC50 = 16 nM). M4K2234 can be used for the investigation of ALK1/2-mediated biological processes and related diseases such as diffuse midline glioma (DMG) and fibrodysplasia ossificans progressiva (FOP).
    M4K2234
  • HY-N0546
    Ligustroflavone
    Inhibitor 99.90%
    Ligustroflavone is an orally active flavonoid compound. Ligustroflavone can be extracted from Ligustrum lucidum. Ligustroflavone antagonizes the calcium-sensing receptor (CaSR), inhibits the RIPK1/RIPK3/MLKL pathway, and downregulates TGF-β/Smad signaling. Ligustroflavone regulates calcium metabolism, protects bone tissue, reduces cerebral ischemic injury, and inhibits liver fibrosis. Ligustroflavone can be used in the study of diabetic osteoporosis, ischemic stroke, and liver fibrosis.
    Ligustroflavone
  • HY-P990993
    Emugrobart
    98%
    Emugrobart (GYM-329, RG6237, RG-70240) is a humanized IgG1κ antibody targeting myostatin (Myostatin; GDF8). Emugrobart binds to pro-myostatin and latent myostatin, blocking their cleavage into mature myostatin; it also has a clearance function, which transports bound myostatin for degradation and allows for cyclic reuse. Emugrobart enhances muscle strength in mouse models of muscle atrophy and increases muscle mass in cynomolgus monkeys. Emugrobart can be used in research on spinal muscular atrophy and facioscapulohumeral muscular dystrophy.
    Emugrobart
  • HY-100444
    SIS3 free base
    Inhibitor 98.02%
    SIS3 free base is a potent and selective inhibitor of Smad3 phosphorylation. SIS3 free base inhibits the myofibroblast differentiation of fibroblasts by TGF-β1. SIS3 free base does not affect the phosphorylation of Smad2.
    SIS3 free base
  • HY-P990957
    Ficerafusp alfa
    Inhibitor 99.71%
    Ficerafusp alfa (BCA-101) is a bispecific antibody targeting EGFR and TGFβ, with a Kd of 2.58 nM against EGFR and a Kd of 61.3 nM against TGFβ1. Ficerafusp alfa binds to EGFR, inhibits EGFR phosphorylation, blocks EGF-dependent cell proliferation, and mediates antibody-dependent cellular cytotoxicity against EGFR-positive tumor cells. Ficerafusp alfa sequesters TGFβ via its TGFβRII ECD domain, neutralizes the activity of TGFβ and TGFβ1, and blocks TGFβ-dependent processes, including epithelial-mesenchymal transition, cell invasion, and differentiation of inducible regulatory T cells. Ficerafusp alfa is applicable to research related to head and neck squamous cell carcinoma, advanced solid tumors, squamous non-small cell lung cancer, anal squamous cell carcinoma, colorectal cancer, and pancreatic cancer.
    Ficerafusp alfa
  • HY-W014841
    Sodium hippurate, 98%
    Activator 99.91%
    Sodium hippurate, 98% is an orally active metabolite. Sodium hippurate, 98% can be produced by intestinal microorganisms from the metabolism of polyphenols, benzoic acid. Sodium hippurate, 98% decreases NRF2, MMP9 and leads to ROS accumulation. Sodium hippurate, 98% activates TGFβ/SMAD signaling. Sodium hippurate, 98% improves hyperuricemia and colitis. Sodium hippurate, 98% can also be used in cardiovascular disease research. .
    Sodium hippurate, 98%
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity