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-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%
  • HY-N0168A
    (Rac)-Hesperetin
    Inhibitor 99.28%
    (Rac)-Hesperetin is the racemate of Hesperetin (HY-N0168), an orally active multi-target inhibitor. (Rac)-Hesperetin exhibits significant anti-tumor and anti-inflammatory activities by blocking the TGF-β1-mediated Fyn/RhoA signaling axis and the TLR4-MyD88-NF-κB inflammatory pathway. (Rac)-Hesperetin inhibits the formation of actin stress fibers and the migration and invasion of cancer cells, and is suitable for triple-negative breast cancer research. In inflammation models, (Rac)-Hesperetin effectively alleviates lung injury by reducing the release of pro-inflammatory mediators and regulating the activity of oxidative stress enzymes, and is suitable for acute lung injury research. (Rac)-Hesperetin also interferes with the entry and early replication processes of channel catfish virus, inhibits viral gene expression and progeny virus production, thereby protecting cells from virus-induced cytopathic effects.
    (Rac)-Hesperetin
  • HY-147025
    (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
    Inhibitor 98.62%
    (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. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine can be used for research on prostate cancer and other cancers.
    (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
  • HY-P5542
    Vicatertide
    Inhibitor 99.24%
    Vicatertide (SB-01, Peniel 2000) is a polypeptide with both competitive inhibitory activity against TGF-β1 and selective inhibitory activity against human factor XIa (hFXIa, with a Ka of 80 nM for hFXIa). Vicatertide binds allosterically to the two binding sites of dimeric hFXI/hFXIa, while directly binding to activated TGF-β1, selectively blocking the Smad1/5/8 pathway and maintaining low-level activation of the Smad2 pathway to enhance the synthesis of type Ⅱ collagen and aggrecan. Vicatertide inhibits thrombus formation in arteriovenous thrombosis models, and also reduces thrombus weight and thrombus incidence in mouse lung cancer models. Vicatertide can be used for research on degenerative disc disease and thrombosis-related diseases.
    Vicatertide
  • HY-142118
    Trabedersen
    Inhibitor
    Trabedersen (AP 12009) is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen 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 exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma.
    Trabedersen
  • HY-N6082
    Rhein 8-O-β-D-Glucopyranoside
    99.81%
    Rhein 8-O-β-D-Glucopyranoside is an orally active glycoside found in Rhubarb. Rhein 8-O-β-D-Glucopyranoside attenuates high glucose-induced apoptosis, recovers altered lincRNA ANRIL and let-7a expression, reverses high glucose-altered Bcl-2 and cleaved caspase-3 protein expression, and inhibits TGF-β1/Smad signaling. Rhein 8-O-β-D-Glucopyranoside accelerates Sennoside A (HY-N0365) metabolism, stimulates sennoside A purgative activity. Rhein 8-O-β-D-Glucopyranoside inhibits bacterial biofilm formation, suppresses its virulence gene expression, and exerts antibacterial activity. Rhein 8-O-β-D-Glucopyranoside can be used for the research of diabetic nephropathy, constipation, and infection.
    Rhein 8-O-β-D-Glucopyranoside
  • HY-121246
    Fluorofenidone
    Inhibitor 99.78%
    Fluorofenidone (AKF-PD) is an orally active compound with anti-fibrotic, antioxidant, and anti-inflammatory pharmacological effects. Fluorofenidone downregulates the expression of ACSL4, upregulates GPX4 expression and inhibits the NF-κB signaling pathway to alleviate inflammation and fibrosis. Fluorofenidone ameliorates cholestasis and fibrosis by inhibiting hepatic Erk/-Egr-1 signaling and Tgfβ1/Smad pathway in mice. Fluorofenidone demonstrates protective effects against chronic lung injury in mice. Fluorofenidone can be used for the study of chronic obstructive pulmonary disease (COPD), pulmonary interstitial fibrosis (PIF) and non-small cell lung cancer (NSCLC).
    Fluorofenidone
  • HY-16268A
    Kartogenin sodium
    Activator 99.84%
    Kartogenin (KGN) sodium is an inducer of chondrogenic tissue formation (EC50: 100 nM). Kartogenin sodium 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 sodium also promotes tendon-bone junction (TBJ) wound healing by stimulating collagen synthesis. Kartogenin sodium 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 sodium promotes cartilage repair, coordinates limb development, and is also used in osteoarthritis (OA) research.
    Kartogenin sodium
  • HY-112247
    SR 16832
    Activator 99.58%
    SR 16832 is a dual-site covalent, orthosteric and allosteric PPARγ antagonist. SR 16832 activates the TGF-β signaling pathway and upregulates the expression of Vimentin and Fibronectin (Fibronectin). SR 16832 is toxic to bronchial epithelium. SR 16832 can be used in research related to type 2 diabetes and pulmonary fibrosis.
    SR 16832
  • HY-P10242
    Myostatin inhibitory peptide 7
    Inhibitor 98.46%
    Myostatin inhibitory peptide 7 is a 23 amino acids peptide, which is derived from amino acids 21 to 43 of the mouse myostatin prodomain. Myostatin inhibitory peptide 7 inhibits myostatin with a Kd of 29.7 nM. Myostatin inhibitory peptide 7 can be used for researches of muscle atrophic disorders.
    Myostatin inhibitory peptide 7
  • HY-109179
    Itacnosertib
    Inhibitor 99.06%
    Itacnosertib (TP-0184) is the inhibitor for FLT3, ACVR1 (ALK2, IC50=8 nM) and JAK2 (IC50=8540 nM). Itacnosertib exhibits anti-leukemic activity.
    Itacnosertib
  • HY-N0363
    (+)-Columbianetin
    Activator 99.04%
    (+)-Columbianetin ((S)-Columbianetin) acts as an inhibitor of JNK/ERK. (+)-Columbianetin inhibits UVA-induced phosphorylation of JNK and ERK, reduces the production of MMP-1, reverses UVA-induced Collagen (HY-NP003) degradation, and alleviates UVA-mediated inhibition of Smad2/3 phosphorylation and translocation. (+)-Columbianetin regulates the AP-1 and ASK1-MAPK signaling pathways, inhibits the production of ROS and blocks sub-G1 cell cycle arrest. (+)-Columbianetin is applicable to research related to skin aging.
    (+)-Columbianetin
  • HY-N0439R
    Asiaticoside (Standard)
    Modulator
    Asiaticoside (Standard) is the analytical standard of Asiaticoside. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N4107
    Phyllanthin
    Inhibitor 99.97%
    Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
    Phyllanthin
  • HY-142042
    3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles
    Inhibitor 99.84%
    3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles is an inhibitor for bone morphogenetic protein 2 (BMP2) with an IC50 of 2.2 μM. 3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles is inhibitor for mitogen-activated protein kinase 1 (MEK1). 3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles exhibits anti-inflammatory and neuroprotective activity in EAE mouse model.
    3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles
  • HY-P990733
    Cibotercept
    Inhibitor 99.85%
    Cibotercept (KER-012) is a novel, modified, investigational activin receptor type IIB (ActRIIB) ligand trap designed to target select TGF-β ligands, including activins A and B, GDFs 8 and 11, to rebalance the defective activin receptor type II signaling observed in PAH.
    Cibotercept
  • HY-W142432
    Perfluoroundecanoic acid
    Activator 99.85%
    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
  • HY-B0673S
    Pirfenidone-d5
    Inhibitor 98.88%
    Pirfenidone-d5 (AMR69-d5) is a deuterium labeled Pirfenidone. Pirfenidone 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-d<sub>5</sub>
  • HY-P0118
    Disitertide
    Inhibitor 98.03%
    Disitertide (P144) is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) is also a PI3K inhibitor and an apoptosis inducer.
    Disitertide
  • HY-160215
    GFH018
    Modulator 98.59%
    GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC50 of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma.
    GFH018
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity