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-162405
    Smad2/3-IN-1
    Inhibitor
    Smad2/3-IN-2 (Compound 27) is an inhibitor for TGF-β-dependent Smad2/3 and IL-4-dependent STAT6 signaling pathway, with IC50s of 90 and 20 nM, respectively.
    Smad2/3-IN-1
  • 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-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-161398
    TGFβRII-IN-3
    Inhibitor
    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 highly selective small-molecule inhibitor targeting Activin receptor type 1 (ALK2, also known as ACVR1). It blocks the SMAD1/5 signaling pathway mediated by ALK2/ALK1, thereby effectively suppressing downstream phosphorylation events induced by BMP and activin A. In the NanoBRET cellular model, CDD-2789 exhibits an inhibitory IC50 of 0.54 µM against ALK2. CDD-2789 holds promise for research on ALK2-related diseases, including diffuse intrinsic pontine glioma (DIPG), ependymoma, endometrial cancer, melanoma, non–small cell lung cancer, colorectal cancer, and pancreatic cancer.
    CDD-2789
  • 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>
  • HY-N0038R
    Alantolactone (Standard)
    Activator
    Alantolactone (Standard) is the analytical standard of Alantolactone. This product is intended for research and analytical applications. Alantolactone is a selective STAT3 inhibitor, with potent anticancer activity. Alantolactone induces apoptosis in cancer.
    Alantolactone (Standard)
  • HY-N0101R
    Neohesperidin (Standard)
    Inhibitor
    Neohesperidin (Standard) is the analytical standard of Neohesperidin. This product is intended for research and analytical applications. Neohesperidin is a flavonoid compound found in high amounts in citrus fruits with anti-oxidant and anti-inflammatory effects.
    Neohesperidin (Standard)
  • HY-151275
    ALK5-IN-28
    Inhibitor
    ALK5-IN-28 (compound Ex-05) is a selective ALK-5 inhibitor (IC50≤10 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-28 has the potential to inhibit growth of tumour in vivo. ALK5-IN-28 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
    ALK5-IN-28
  • HY-151282
    ALK5-IN-32
    Inhibitor
    ALK5-IN-32 (compound EX-09) is a selective ALK-5 inhibitor (10 nM<IC50<100 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-32 has the potential to inhibit growth of tumour in vivo. ALK5-IN-32 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
    ALK5-IN-32
  • HY-115577
    Mitochonic acid 35
    Inhibitor
    Mitochonic acid 35 is an IAA analogue with cytoprotective effects.
    Mitochonic acid 35
  • HY-P10242A
    Myostatin inhibitory peptide 7 TFA
    Inhibitor
    Myostatin inhibitory peptide 7 TFA is a 23 amino acids peptide, which is derived from amino acids 21 to 43 of the mouse myostatin prodomain. Myostatin inhibitory peptide 7 TFA inhibits myostatin with a Kd of 29.7 nM. Myostatin inhibitory peptide 7 TFA can be used for researches of muscle atrophic disorders.
    Myostatin inhibitory peptide 7 TFA
  • HY-120973
    Butaprost free acid
    Inhibitor
    Butaprost free acid is a selective prostaglandin E receptor (EP2) agonist with an EC50 of 33 nM and a Ki of 2.4 μM for murine EP2 receptor. Butaprost free acid is less activity against murine EP1, EP3 and EP4 receptors. Butaprost free acid attenuates fibrosis by hampering TGF-β/Smad2 signalling.
    Butaprost free acid
  • HY-W707119
    RepSox hydrochloride
    Inhibitor
    RepSox hydrochloride is a potent and selective inhibitor of transforming growth factor-β receptor I/activin-like kinase 5 (TGF-β-RI/ALK5). RepSox hydrochloride inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox hydrochloride can be used in the study of obesity and related metabolic diseases such as type 2 diabetes.
    RepSox hydrochloride
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity