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-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
  • HY-176737
    TGF-β1/Smad-IN-1
    		Inhibitor
    TGF-β1/Smad-IN-1 (compound C9) is a potent TGF-β1/Smad inhibitor. TGF-β1/Smad-IN-1 inhibits the expression of fibrosis markers (α-SMA and COL1A1) induced by TGF-β1. TGF-β1/Smad-IN-1 shows antifibrotic effects. TGF-β1/Smad-IN-1 has the potential for the research of hepatic fibrosis.
    TGF-β1/Smad-IN-1
  • HY-10321G
    PD173074 (GMP)
    		Inhibitor
    PD173074 GMP is PD173074 (HY-10321) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. PD173074 is an orally active FGFR inhibitor that targets the transphosphorylation of FGFR1 and FGFR2 and blocks the FGF signaling pathway. By reducing the phosphorylation level of SMAD2 and altering the expression of Nodal/Activin target genes, PD173074 eliminates endothelial differentiation potential, thereby inhibiting the formation of capillary-like structures. PD173074 blocks the proliferation and colony formation of tumor cells and increases intratumoral cell apoptosis. PD173074 successfully reverses FGF-2-induced chemoresistance to enhance the effect of cisplatin (HY-17394) in small cell lung cancer models. PD173074 can be applied to research related to critical limb ischemia and small cell lung cancer.
    PD173074 (GMP)
  • HY-N1326
    Santamarine
    		98.85%
    Santamarine (Santamarin; Balchanin) is a sesquiterpene lactone found in Artemisia scoparia. Santamarine shows anti-inflammatory, antioxidant, anticancer and anti-photoaging activities. Santamarine suppresses UVA-induced phosphorylation of JNK and p38 MAPK, nuclear translocation of phosphorylated c-Fos and c-Jun, and AP-1-mediated MMP-1 transcription and secretion. Santamarine suppresses NF-κB signaling, iNOS, COX-2, TNF-α, and IL-1β production. Santamarine inhibits thioredoxin reductase activity, induces ROS production, mitochondrial apoptosis, G2/M cell cycle arrest, and DNA damage, and reduces cancer cell growth. Santamarine can be used for the photoaging, inflammatory diseases and cancer.
    Santamarine
  • HY-181823
    HOXA1-IN-1
    		Inhibitor
    HOXA1-IN-1 is a HOXA1 inhibitor. HOXA1-IN-1 downregulates HOXA1 protein levels, suppresses its transcriptional activity, and alters the expression of its downstream target genes. HOXA1-IN-1 induces DNA damage and apoptosis in cancer cells. HOXA1-IN-1 exhibits antitumor efficacy in xenograft models of colorectal cancer and triple-negative breast cancer. HOXA1-IN-1 shows synergistic activity in combination with Cisplatin (HY-17394). HOXA1-IN-1 can be used for the research of colorectal cancer and triple-negative breast cancer.
    HOXA1-IN-1
  • HY-126675G
    AS2863619 (GMP)
    		Activator
    AS2863619 GMP is AS2863619 (HY-126675) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AS2863619 is an orally active CDK8/19 inhibitor that also inhibits BMP2, MDA5 and RIG-I receptors. AS2863619 targets Stat5a-CDK8/19 to promote the differentiation of CD4+ T cells into regulatory T cells and induce FOXP3 expression, thereby restoring immune homeostasis and establishing transplant immune tolerance. AS2863619 also enhances the BMP2/SMAD signaling pathway to promote osteogenic differentiation and inhibit adipogenic differentiation. AS2863619 exerts osteoprotective effects by alleviating inflammation-induced impairment of osteogenic function and inducing neutrophil apoptosis (apoptosis). AS2863619 can be applied to research in related fields such as periodontitis-induced bone defects.
    AS2863619 (GMP)
  • HY-162405
    STAT6-IN-12
    		Inhibitor
    STAT6-IN-12 is a potent STAT6 inhibitor with an IC50 of 50 nM. STAT6-IN-12 also inhibits Smad2/3 with an IC50 of 68 nM. STAT6-IN-12 inhibits TGFβ-dependent Smad2/3 signaling pathway, IL-4-dependent STAT6 signaling pathway, and cellular inflammatory responses. STAT6-IN-12 can be used for the research of inflammation.
    STAT6-IN-12
  • HY-P3971
    H-Leu-Ser-Lys-Leu-OH
    		Inhibitor
    H-Leu-Ser-Lys-Leu-OH (LSYL) is a latency-associated peptide at the amino terminus of LAP, with inhibitory effect on TGF-β1 activation. H-Leu-Ser-Lys-Leu-OH, binding with KRFK (HY-P3970), can block the signal transduction of TGF-β1, and prevent the progression of hepatic damage and fibrosis.
    H-Leu-Ser-Lys-Leu-OH
  • HY-B0252S3
    Hydrochlorothiazide-15N2,13C,d2
    		Inhibitor
    Hydrochlorothiazide-15N2,13C,d2 is 15N and deuterated labeled Hydrochlorothiazide (HY-B0252). 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.
    Hydrochlorothiazide-<sup>15</sup>N<sub>2</sub>,<sup>13</sup>C,d<sub>2</sub>
  • HY-E70299
    ST3 β-Gal α-2,3-Sialyltransferase 5
    		Inhibitor
    ST3 β-Gal α-2,3-Sialyltransferase 5 (ST3GAL5) is a glycosphingolipid (GSL) biosynthetic enzyme that can inhibit TGF-β-induced epithelial-mesenchymal transition (EMT), invasion, and metastasis both in vivo and in vitro. ST3 β-Gal α-2,3-Sialyltransferase 5 can be used in cancer research.
    ST3 β-Gal α-2,3-Sialyltransferase 5
  • HY-169026
    DCN1-IN-2
    		Inhibitor
    DCN1-IN-2 is a DCN1 inhibitor with an IC50 value of 2.96 nM. DCN1-IN-2 can alleviate Ang II/TGFβ-induced activation of cardiac fibroblasts. DCN1-IN-2 can reduce ISO-induced cardiac fibrosis and remodeling in mice by selectively inhibiting cullin 3.
    DCN1-IN-2
  • HY-182038
    TGF-β1/Smad3-IN-2
    		Inhibitor
    TGF-β1/Smad3-IN-2 is an orally active antifibrotic agent. TGF-β1/Smad3-IN-2 has high affinity for VDR and can inhibit the TGFβ/SMAD3 signaling pathway. TGF-β1/Smad3-IN-2 inhibits hepatic stellate cell activation, reduces extracellular matrix deposition, and alleviates liver fibrosis in a bile duct ligation mouse model. TGF-β1/Smad3-IN-2 can be used for the research of liver fibrosis.
    TGF-β1/Smad3-IN-2
  • HY-P10414
    Klotho-derived peptide 1
    		Inhibitor
    Klotho-derived peptide 1 (KP1 human) blocks TGF-β/TGF-β receptor 2 interaction, inhibits TGF-β-induced activation of Smad2/3 and mitogen-activated protein kinase (MAPK), and exhibits anti-fibrotic and kidney protective effects in mouse model.
    Klotho-derived peptide 1
  • HY-P10359
    TAT-QFNP12
    		Inhibitor
    TAT-QFNP12 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
  • HY-132187S
    Sphingosylphosphorylcholine-d9
    		Inducer 99.0%
    Sphingosylphosphorylcholine-d9 is deuterium labeled Sphingosylphosphorylcholine.
    Sphingosylphosphorylcholine-d<sub>9</sub>
  • HY-181431
    PXS 64
    		Inducer
    PXS 64, a mannose-6-phosphate (M6P) analogue. a lipophilic prodrug of PXS 25 (HY-181430). PXS 64 is an effective anti-fibrotic agent by inhibiting the activation of latent TGF-β1. PXS64, inhibits fibrosis via TGF-β1 pathway in human lung fibroblasts. PXS 64 reduces TGFβ-mediated collagen IV, fibronectin, MCP-1, and phospho-smad2 expression in kidney cells. PXS 64 reduces collagen deposition in dermal scar fibroblasts. PXS 64 can be used for the research of chronic kidney disease, idiopathic pulmonary fibrosis, scarring.
    PXS 64
  • HY-N0168AR
    (Rac)-Hesperetin (Standard)
    		Inhibitor
    (Rac)-Hesperetin (Standard) is the analytical standard of (Rac)-Hesperetin. This product is intended for research and analytical applications. (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 (Standard)
  • HY-175971
    PDE1-IN-10
    		Inhibitor
    PDE1-IN-10 is a potent and sekective Phosphodiesterase 1 (PDE1) inhibitor with an IC50 of 5 nM. PDE1-IN-10 can suppress TGF-β/Smad-MAPK signaling and exhibit antifibrotic effects. PDE1-IN-10 can be used for the research of idiopathic pulmonary fibrosis.
    PDE1-IN-10
  • HY-P10476A
    Myostatin inhibitory peptide 2 TFA
    		Inhibitor 99.12%
    Myostatin inhibitory peptide 2 (compd 2) TFA is a myostatin inhibitor with a Kd of 35.9 nM. Myostatin inhibitory peptide 2 TFA can be used for researches of muscle atrophic disorders.
    Myostatin inhibitory peptide 2 TFA
  • HY-W701772
    2-Oleoylglycerol-d5
    2-Oleoylglycerol-d5 (2-OG-d5) is the deuterium labeled 2-Oleoylglycerol (HY-W011121). 2-Oleoylglycerol (2-OG) is a lipid found in the diet. It is a GPR119 agonist, with an EC50 value of 2.5 μM in activating hGPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol enhances the inflammatory response of macrophages and promotes fibrosis by activating the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. It also stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. 2-Oleoylglycerol is expected to be used in the research of non-alcoholic steatohepatitis (NASH) .
    2-Oleoylglycerol-d<sub>5</sub>
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Cat. No. Product Name / Synonyms Application Reactivity