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-N6679A
    10,11-Dehydrocurvularin
    		Inhibitor 99.75%
    10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity.
    10,11-Dehydrocurvularin
  • HY-N2199
    Sotetsuflavone
    		Inhibitor
    Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits phosphorylation of PI3K, Akt, mTOR, JNK, and p38 MAPK; modulates expression of Cyclin D1, CDK4, Bcl-2, Bax, cleaved caspases 3/9, MMP-9, TGF-β, STAT3, and β-catenin. Sotetsuflavone induces G0/G1 cell cycle arrest, apoptosis, autophagy, and intracellular ROS elevation, inhibits cancer cell proliferation. Sotetsuflavone inhibits tumor growth in mouse tumor xenograft models. Sotetsuflavone can be used for the research of non-small cell lung cancer and Crohn’s disease.
    Sotetsuflavone
  • HY-170813
    P162-0948
    		Inhibitor
    P162-0948 is a selective CDK8 inhibitor with an IC50 value of 50.4 nM. P162-0948 reduces cell migration and protein expression of EMT-related proteins in A549 human alveolar epithelial cell lines. P162-0948 reduces phosphorylation of Smad, which suggests disruption of the TGF-β/Smad signaling pathway. P162-0948 is promising for research of pulmonary fibrosis.
    P162-0948
  • HY-178821
    ROCK2-IN-12
    		Inhibitor 98.02%
    ROCK2-IN-12 (Compound A25) is a selective ROCK2 inhibitor with an IC50 of 7.0  nM for ROCK2 over ROCK1. ROCK2-IN-12 has potent antifibrotic effects via the TGF-β/Smad and ROCK2/STAT3 signaling pathways. ROCK2-IN-12 significantly reduces collagen deposition and reverses fibrotic progression in Bleomycin (HY-108345)-induced pulmonary fibrosis (PF) mouse models. ROCK2-IN-12 can be used for lung diseases like pulmonary fibrosis research.
    ROCK2-IN-12
  • 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-P10359A
    TAT-QFNP12 acetate
    		Inhibitor
    TAT-QFNP12 acetate is a peptide that blocks the NDRG2-PPM1A binding and reduces Smad2/3 phosphorylation, decreases astrocytic MMP-9 production and BBB disruption after subarachnoid hemorrhage (SAH).
    TAT-QFNP12 acetate
  • HY-P0118A
    Disitertide TFA
    		Inhibitor
    Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide TFA is also a PI3K inhibitor and an apoptosis inducer.
    Disitertide TFA
  • HY-B0252S1
    Hydrochlorothiazid-13C,d2
    		Inhibitor 98.64%
    Hydrochlorothiazid-13C,d2 is the 13C- and 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-<sup>13</sup>C,d<sub>2</sub>
  • HY-161398
    TGFβRII-IN-3
    		Inhibitor 99.51%
    TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) (IC50 = 4.1 μM). TGFβRII-IN-3 inhibits TGFβ signaling by promoting the proteolytic degradation of TGFβ RII. TGFβRII-IN-3 can block endothelial-to-mesenchymal transition and cell migration. TGFβRII-IN-3 can be used in cancer research.
    TGFβRII-IN-3
  • HY-173149
    CDD-2789
    		Inhibitor
    CDD-2789 is a potent and selective ALK2 inhibitor with an IC50 0.54 μM and a Kd of 2.1 nM, respectively. CDD-2789 exhibits >120-fold selectivity over ALK3/5/6. CDD-2789 reduces activin A- and BMP2-induced SMAD1/5 phosphorylation in fibroblasts. CDD-2789 can be used for ALK2-related cancer research.
    CDD-2789
  • HY-156512
    DT-6
    		Inhibitor 99.82%
    DT-6 is an effective TGF-β1 inhibitor. DT-6 inhibits M2 macrophage induced epithelial to mesenchymal transition and invasive migration of cancer cells. DT-6 can be used for cancer diseases research.
    DT-6
  • HY-P11223
    CMF9
    		Inhibitor 98.65%
    CMF9, a cyclic peptide molecule, is an inhibitor of the SMAD2-SMAD4 interaction. CMF9 effectively blocks the formation of the heterodimeric complex of SMAD2 and SMAD4 by inhibiting the phosphorylation of SMAD2. CMF9 has no effect on the phosphorylation of SMAD3 or SMAD1/5/8. CMF9 downregulates the expression of fibrotic markers α-SMA and COL1A1. CMF9 exhibits potent anti-fibrotic effects in mouse models by promoting the degradation of pathological extracellular matrix (ECM) and inhibiting inflammation. CMF9 can be used for the study of liver fibrosis.
    CMF9
  • HY-N1584AR
    Halofuginone hydrobromide (Standard)
    		Inhibitor
    Halofuginone (hydrobromide) (Standard) is the analytical standard of Halofuginone (hydrobromide). 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.
    Halofuginone hydrobromide (Standard)
  • HY-P990720
    Elritercept
    		Inhibitor
    Elritercept (KER-050) is a recombinant fusion protein comprising a modified activin receptor type IIA extracellular domain fused to a human IgG1 Fc. Elritercept inhibits activin A and other select TGF-β superfamily ligands.
    Elritercept
  • HY-158821A
    ISTH0036 sodium
    		Inhibitor
    ISTH0036 sodium is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 sodium suppresses TGF-β2 expression, reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-to-mesenchymal transition, and inhibits angiogenesis while promoting bleb survival. ISTH0036 sodium exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 sodium can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases.
    ISTH0036 sodium
  • HY-N9912
    Physalin D
    		Inhibitor 98.21%
    Physalin D is isolated from the aerial parts of Physalis angulate. Physalin D displays considerable cytotoxicity against several cancer cell lines, showing IC50 values in the range of d 0.28 to 2.43 microg/mL. Physalin D has the potential for the cancer disease.
    Physalin D
  • HY-N1584R
    Halofuginone (Standard)
    		Inhibitor
    Halofuginone (Standard) is the analytical standard of Halofuginone. This product is intended for research and analytical applications. Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
    Halofuginone (Standard)
  • HY-132187S1
    Sphingosylphosphorylcholine-d7
    		Inducer 99.90%
    Sphingosylphosphorylcholine-d7 is the deuterium labeled Sphingosylphosphorylcholine (HY-132187).
    Sphingosylphosphorylcholine-d<sub>7</sub>
  • HY-N0168AS
    (Rac)-Hesperetin-d3
    		Inhibitor
    (Rac)-Hesperetin-d3 is the deuterium labeled (Rac)-Hesperetin. (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-d<sub>3</sub>
  • HY-116084S1
    Trimethylamine-N-oxide-13C3
    		Activator
    Trimethylamine-N-oxide-13C3 is the 13C-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.
    Trimethylamine-N-oxide-<sup>13</sup>C<sub>3</sub>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity