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-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-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-P10476A
    Myostatin inhibitory peptide 2 TFA
    Inhibitor
    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-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-P10634
    P17 Peptide
    P17 Peptide is a human TGF-β1 inhibitory peptide. P17 Peptide can block woodchuck TGF-β1 activity.
    P17 Peptide
  • 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 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-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-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-100830A
    NCB-0970
    Control
    NCB-0970 is the negative control of NCB-0846 (HY-100830). NCB-0846 is an orally active, selective inhibitor for Wnt, that inhibits Traf2- and Nck-interacting kinase (TNIK) with an IC50 of 21 nM. NCB-0846 blocks TGF-β signaling pathway by inhibiting SMAD2/3 phosphorylation and nuclear translocation.
    NCB-0970
  • HY-146056
    Anabolic agent-1
    Activator
    Compounds, as a new type of bone morphogenetic protein-2 up regulator, can not only correct the bone loss in patients, but also have a wide range of clinical applicability.
    Anabolic agent-1
  • 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-137063
    (+)-ITD-1
    Inhibitor
    (+)-ITD-1 is an inhibitor for TGF-β, that inhibits the TGF-β2 with an IC50 of 0.46 μM. (+)-ITD-1 promotes the degradation of TGF-b type II receptor (TGFBR2) and the differentiation of cardiomyocyte, and inhibits the mesoderm formation in the early differentiation stage of mouse embryonic stem cells (mESCs).
    (+)-ITD-1
  • HY-107614G
    1-Oleoyl lysophosphatidic acid (sodium) (GMP)
    Agonist
    1-Oleoyl lysophosphatidic acid sodium (GMP) is a GMP-grade 1-Oleoyl lysophosphatidic acid sodium that can be used as an auxiliary reagent in cell therapy. 1-Oleoyl lysophosphatidic acid sodium can stimulate neuronal differentiation in neural progenitor cells from mice or rats, and it also promotes the differentiation of human adipose-derived mesenchymal stem cells into myofibroblast-like cells in vitro by activating the autocrine TGF-β1-Smad signaling pathway.
    1-Oleoyl lysophosphatidic acid (sodium) (GMP)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity