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-N0559R
    Kirenol (Standard)
    		Inhibitor
    Kirenol (Standard) is the analytical standard of Kirenol (HY-N0559). This product is intended for research and analytical applications. Kirenol is a diterpenoid compound, an orally active apoptosis inducer and signaling pathway regulator, with a Kd value of 5.47 μM against the target CK2. Kirenol promotes the cleavage of Bid into tBid, regulates the protein levels/phosphorylation of Bax, Bcl-2, p53 and p21, and induces caspase-independent apoptosis, S-phase cell cycle arrest, ROS accumulation and cytotoxicity in cancer cells. Kirenol activates the CK2/AKT and AMPK-mTOR-ULK1 pathways, inhibits the signaling of NF-κB, TGF-β/Smads and NLRP3 inflammasome, and regulates the GSK3β, BMP and Wnt/β-catenin pathways. Kirenol induces autophagy, mitophagy and osteoblast differentiation, promotes mitochondrial fusion, and exerts antioxidant, anti-inflammatory, antifibrotic, renoprotective, cardioprotective, neuroprotective and analgesic effects. Kirenol is applicable to research related to chronic myeloid leukemia, ischemic stroke, diabetic nephropathy, heart failure, acute lung injury and osteoporosis.
    Kirenol (Standard)
  • HY-175662
    TGF-β/Smad-IN-2
    		Inhibitor
    TGF-β/Smad-IN-2 is an orally active TGF-β/Smad inhibitor. TGF-β/Smad-IN-2 inhibits TGF-β-induced fibroblast-to-myofibroblast differentiation and collagen deposition, with an IC50 value of 102 μM for collagen reduction in LL29 cells. TGF-β/Smad-IN-2 exerts its effects through modulation of the SMAD3/SMAD7 signaling pathway. TGF-β/Smad-IN-2 reduces lung index in pulmonary fibrosis mice. TGF-β/Smad-IN-2 can be used for the study of pulmonary fibrosis.
    TGF-β/Smad-IN-2
  • HY-126734
    Avenanthramide E
    Avenanthramide E is a collagen synthesis inhibitor. Avenanthramide E inhibits TGF-β-stimulated Collagen synthesis. Avenanthramide E can be used for the research of diabetic nephropathy.
    Avenanthramide E
  • HY-N16980
    (7'E,8S)-2',4,8-Trihydroxy-3-methoxy-2,4'-epoxy-8,5'-neolign-7'-en-7-one
    		Inhibitor
    (7'E,8S)-2',4,8-Trihydroxy-3-methoxy-2,4'-epoxy-8,5'-neolign-7'-en-7-one (compound 4) is a novel neolignan anti-inflammatory agent. (7'E,8S)-2',4,8-Trihydroxy-3-methoxy-2,4'-epoxy-8,5'-neolign-7'-en-7-one has an IC50 of 25.2 μM against TGF-β-induced hepatic stellate cells (HSC-T6). (7'E,8S)-2',4,8-Trihydroxy-3-methoxy-2,4'-epoxy-8,5'-neolign-7'-en-7-one may be related to blocking excessive cell proliferation in the process of liver fibrosis and can be used in the study of liver fibrosis-related diseases. (7'E,8S)-2',4,8-Trihydroxy-3-methoxy-2,4'-epoxy-8,5'-neolign-7'-en-7-one can be naturally extracted from the dried aerial parts of Penthorum chinense Pursh.
    (7'E,8S)-2',4,8-Trihydroxy-3-methoxy-2,4'-epoxy-8,5'-neolign-7'-en-7-one
  • HY-107614G
    1-Oleoyl lysophosphatidic acid sodium (GMP)
    		Activator
    1-Oleoyl lysophosphatidic acid sodium (GMP) is the GMP-grade form of 1-Oleoyl lysophosphatidic acid sodium (HY-107614). GMP-grade small molecules serve as auxiliary reagents in cell therapy. 1-Oleoyl lysophosphatidic acid sodium is a bioactive lipid signaling molecule. 1-Oleoyl lysophosphatidic acid sodium inhibits lysoPLD-catalyzed hydrolysis of lysophosphatidylcholine and FS-3. 1-Oleoyl lysophosphatidic acid sodium activates LPA1 and LPA2, thereby triggering calcium mobilization, NFATc1 translocation, Rho/ROCK activation, Smad2/3 phosphorylation and c-Fos expression. 1-Oleoyl lysophosphatidic acid sodium induces anxiety-like, depression-like and hypoactivity phenotypes, regulates osteoclast cytoskeleton and viability, reduces osteoclast bone resorptive activity, and drives mesenchymal stem cell differentiation into myofibroblast-like cells. 1-Oleoyl lysophosphatidic acid sodium stimulates the secretion of transforming growth factor-β1 and stromal cell-derived factor-1. 1-Oleoyl lysophosphatidic acid sodium is applicable to research related to anxiety, depression and ovarian cancer.
    1-Oleoyl lysophosphatidic acid sodium (GMP)
  • HY-17661
    Depiperazine-DM3189
    		Inhibitor
    Depiperazine-DM3189 is a derivative of LDN193189 (HY-12071). LDN193189 is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.
    Depiperazine-DM3189
  • HY-100113A
    Buloxibutid hydrochloride
    		Inhibitor
    Buloxibutid (AT2 receptor agonist C21) hydrochloride is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a Ki value of 0.4 nM for porcine AT2R. Buloxibutid hydrochloride exerts vasodilatory, anti-inflammatory, antifibrotic (promoting the expression of collagenase MMP-13) and tissue repair effects mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway and inflammatory NF-κB pathway. Buloxibutid hydrochloride can be used in research related to idiopathic pulmonary fibrosis, hypertension, systemic sclerosis and other conditions.
    Buloxibutid hydrochloride
  • HY-175205
    TGF-β2-IN-1
    		Inhibitor
    TGF-β2-IN-1 is a selective TGF-β2 inhibitor. TGF-β2-IN-1 exhibits potent antiproliferative effects on HCT-116, Caco-2 and HT-29 with IC50 values of 6.84, 10.21, and 9.47 μM, respectively. TGF-β2-IN-1 inhibits TGF-β2 signaling in a dose-dependent manner by suppressing both receptor and cytokine expression.TGF-β2-IN-1 can be used for the study of colorectal cancer.
    TGF-β2-IN-1
  • HY-170540
    NOX4-IN-1
    		Inhibitor
    NOX4-IN-1 (Compound 14m) is the inhibitor for NADPH oxidase 4 (NOX4), and blocks the generation of ROS. NOX4-IN-1 inhibits TGF-β1/Smad signaling pathway, decreases the expression of fibrosis-related proteins. NOX4-IN-1 inhibits the cell migration of NRK-49F.
    NOX4-IN-1
  • HY-179378
    XRF-1021
    		Inhibitor
    XRF-1021 is an orally active HIPK2 inhibitor (IC50 = 0.18 μM). XRF-1021 reduces the expression of fibrotic markers in TGF-β1 stimulated NRK-49F and HK-2 cells, including Fibronectin, Collagen I and α-SMA. XRF-1021 blocks TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch signaling. XRF-1021 reduces renal injury and fibrosis in vivo. XRF-1021 can be used for the research of chronic kidney disease.
    XRF-1021
  • HY-P992311
    Anti-USAG-1 Antibody
    Anti-USAG-1 Antibody is a monoclonal antibody that targets SOSTDC1. Anti-USAG-1 Antibody can be used in ELISA, FACS, and functional assays.
    Anti-USAG-1 Antibody
  • HY-181808
    HSF1/AMPK activator 1
    		Inhibitor
    HSF1/AMPK activator 1 is a compound that modulates the HSF1/AMPK axis and the TGF-β1/Smad signaling pathway. HSF1/AMPK activator 1 exhibits anti-hepatic fibrosis activity and metabolic stability. HSF1/AMPK activator 1 inhibits fibrosis formation and cell proliferation in activated hepatic stellate cells. HSF1/AMPK activator 1 alleviates liver injury and hepatic fibrosis symptoms in fibrotic mice. HSF1/AMPK activator 1 is applicable to research related to hepatic fibrosis.
    HSF1/AMPK activator 1
  • HY-P99100A
    Visugromab (Powder)
    		Inhibitor
    Visugromab (CTL-002) (Powder) is a GDF-15 neutralizing IgG4 mAb. Visugromab (Powder) has synergistic anticancer activity with the anti-PD1 antibody Nivolumab (HY-P9903) and can effectively act on PD-1/PD-L1 relapsed/refractory metastatic solid tumors. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).
    Visugromab (Powder)
  • HY-145721C
    Mongersen sodium scrambled negative control
    Mongersen sodium scrambled negative control is the sequence scrambled negative control of Mongersen sodium.
    Mongersen sodium scrambled negative control
  • HY-P992304
    Anti-SOSTDC1 Antibody
    Anti-SOSTDC1 Antibody is a monoclonal antibody that targets SOSTDC1. Anti-SOSTDC1 Antibody can be used in ELISA, FACS, and functional assays.
    Anti-SOSTDC1 Antibody
  • HY-159692C
    AZD8701 sodium scrambled negative control
    		Inhibitor
    AZD8701 sodium scrambled negative control is the sequence scrambled negative control of AZD8701 sodium.
    AZD8701 sodium scrambled negative control
  • HY-W142432S
    Perfluoroundecanoic acid-13C7
    Perfluoroundecanoic acid-13C7 is the 13C-labeled Perfluoroundecanoic acid (HY-W142432). Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation.
    Perfluoroundecanoic acid-<sup>13</sup>C<sub>7</sub>
  • HY-P992410
    MEDI-579
    		Inhibitor
    MEDI-579 is a fully human monoclonal antibody against PAI-1, with a KD value of 6 pM for human PAI-1 and 105 pM for rat PAI-1. MEDI-579 restores renal plasmin activity and inhibits PAI-1-mediated intracellular signal transduction. MEDI-579 reduces albuminuria, glomerulosclerosis severity, TGF-β1 expression level, and phosphorylated Smad2 level induced in diabetic mice. MEDI-579 decreases the levels of active PAI-1 in plasma and kidneys, and increases plasma plasmin level in a mouse model of lupus nephritis. MEDI-579 can be used in research related to diabetic nephropathy and lupus nephritis. The recommended isotype control is human IgG1 kappa (HY-P99001).
    MEDI-579
  • HY-N1584BR
    Halofuginone hydrochloride (Standard)
    		Inhibitor
    Halofuginone (hydrochloride) (Standard) is the analytical standard of Halofuginone (hydrochloride). This product is intended for research and analytical applications. 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[4].
    Halofuginone hydrochloride (Standard)
  • HY-183067
    TAS1440
    		Activator
    TAS1440 is an orally active LSD1/KDM1A inhibitor with a human IC50 of 4.8 nM. TAS1440 non-covalently binds to the histone H3-binding pocket of LSD1, inhibiting demethylase activity and disrupting repressive complexes with INSM1 and SMAD2. TAS1440 activates tumor-suppressive TGF-β and NOTCH signaling pathways via transcriptional reprogramming. TAS1440 can be used for the research of small cell lung cancer, specifically the SCLC-A subtype.
    TAS1440
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