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-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-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-P10899
    ETTAC-2
    Inhibitor 98.22%
    ETTAC-2 is a LRG1 PROTAC degrader. ETTAC-2 promotes ubiquitination and degradation of LRG1 (DC50 of 8.38 µM). ETTAC-2 inhibits the TGF-β-Smad3 signaling pathway and diminishes the secretion of fibrosis-associated proteins. ETTAC-2 attenuates the progression of renal fibrosis.
    ETTAC-2
  • 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-N2013
    Aristolactam I
    Activator 99.31%
    Aristolactam I is an AQP1 inhibitor and Aristolochic acid I metabolite. Aristolactam I can be isolated from Aristolochia plants. Aristolactam I downregulates Twist1 expression, increases E-cadherin expression, and activates the TGF-β/Smad signaling pathway. Aristolactam I has anticancer activity against breast cancer. Aristolactam I is nephrotoxic. Aristolactam I is mainly used in the study of breast cancer and kidney diseases such as renal interstitial fibrosis.
    Aristolactam I
  • HY-P990426
    Anti-GREM1/Gremlin Antibody
    98.59%
    The Anti-GREM1/Gremlin Antibody is a humanized antibody expressed in CHO that targets GREM1/Gremlin. The Anti-GREM1/Gremlin Antibody has a huIgG4SP heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for the Anti-GREM1/Gremlin Antibody can refer to Human IgG4 kappa, Isotype Control (HY-P99003).
    Anti-GREM1/Gremlin Antibody
  • HY-W108953A
    Myristoyl tetrapeptide-12 dihydrochloride
    Activator 99.88%
    Myristoyl tetrapeptide-12 dihydrochloride is a peptide containing lysine and alanin. Myristoyl tetrapeptide-12 dihydrochloride is utilized as hair cair preparations agent in cosmetics industry.
    Myristoyl tetrapeptide-12 dihydrochloride
  • HY-145721
    Mongersen
    Inhibitor
    Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen can attenuate Crohn's disease-like experimental colitis in mice.
    Mongersen
  • HY-149414
    MY-673
    Inhibitor 98.60%
    MY-673 is a colchicine binding site inhibitor (CBSI), that inhibits tubulin polymerization. MY-673 inhibits the ERK signaling pathway, which in turn affects SMAD4 protein expression levels in the TGF-β/SMAD pathway. MY-673 inhibited cell proliferation, migration and induced apoptosis in vivo and in vitro.
    MY-673
  • HY-N6896
    Isoviolanthin
    Inhibitor 99.66%
    Isoviolanthin is a flavonoid glycoside. Isoviolanthin can be extracted from Dendrobium officinale. Isoviolanthin has a strong affinity for binding to KDM6B, CHAC2, ESCO2, and IPO4. Isoviolanthin decreases MMP-2 and MMP-9. Isoviolanthin inhibits TGF-β/Smad and PI3K/Akt/mTOR signaling pathways. Isoviolanthin increases Fhl3 expression. Isoviolanthin has cytoprotective effects. Isoviolanthin has anticancer activity against hepatocellular carcinoma.
    Isoviolanthin
  • HY-P10242
    Myostatin inhibitory peptide 7
    Inhibitor 99.42%
    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-B0673S
    Pirfenidone-d5
    Inhibitor 98.88%
    Pirfenidone-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-109179A
    Itacnosertib hydrochloride
    Inhibitor 99.43%
    Itacnosertib hydrochloride (TP-0184 hydrochloride) is the inhibitor for FLT3, ACVR1 (ALK2, IC50=8 nM) and JAK2 (IC50=8540 nM). Itacnosertib hydrochloride exhibits anti-leukemic activity.
    Itacnosertib hydrochloride
  • HY-124674A
    CCT365623 hydrochloride
    Activator 98.07%
    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.
    CCT365623 hydrochloride
  • HY-W005379
    DGM
    Inhibitor 99.99%
    DGM is an inhibitor of the TGF-β1/Smad signaling pathway with significant antifibrotic effects. DGM inhibits the epithelial-mesenchymal transition (EMT) process in alveolar epithelial cells and slows the progression of pulmonary fibrosis in vivo by reducing lung inflammation, improving lung function, and decreasing extracellular matrix (ECM) remodeling. DGM can be used in research on idiopathic pulmonary fibrosis (IPF) and EMT-related diseases.
    DGM
  • HY-16268A
    Kartogenin sodium
    Activator 98.25%
    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-14928A
    Lobeglitazone sulfate
    Inhibitor 99.63%
    Lobeglitazone sulfate is a new type of thiazolidinedione. Lobeglitazone sulfate is the orally active agonist for PPAR with EC50 of 137.4 nM and 546.3 nM for PPARγ and PPARα. Lobeglitazone sulfate is the inhibitor for ERK/JNK/Smad/NF-κB signaling pathway. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic and anti-atherosclerotic properties.
    Lobeglitazone sulfate
  • HY-170791
    CIB-L43
    Modulator 99.71%
    CIB-L43 is an orally active TRBP inhibitor (KD = 4.78 nM) and enhances disruption of TRBP-Dicer interactions (IC50 = 2.34 μM). CIB-L43 suppresses oncogenic miR-21 biosynthesis, increasing PTEN and Smad7 expression and inhibiting AKT and TGF-β signaling, thereby reducing HCC cell proliferation and migration.
    CIB-L43
  • HY-B0252S
    Hydrochlorothiazid-d2
    Inhibitor 98.89%
    Hydrochlorothiazid-d2 is the deuterium labeled Hydrochlorothiazide. 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.
    Hydrochlorothiazid-d<sub>2</sub>
  • HY-W803134
    (E/Z)-SIS3 free base
    Inhibitor 99.48%
    E/Z-SIS3 free base exhibits an inhibitory efficacy against smad3, exhibits an anti-fibrotic and anti-inflammatory effect through a TGF-β/smad3 signaling pathway.
    (E/Z)-SIS3 free base
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity