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-N1510
    Kaempferol 3-O-gentiobioside
    Inhibitor 99.88%
    Kaempferol 3-O-gentiobioside is an orally active flavonoid, with a Ka value of 57 µM against human NOTCH1 and an IC50 value of 50 μM against α-glucosidase. Kaempferol 3-O-gentiobioside inhibits the NOTCH signaling pathway. It downregulates the expression of TLR4 and NLRP3, and suppresses the activation and nuclear translocation of NF-κB. Kaempferol 3-O-gentiobioside inhibits the expression of MUC5AC, reduces nitrite and ROS levels, and attenuates excessive mucus secretion. It exhibits antibacterial activity, reducing the formation and growth of MRSA biofilms. Kaempferol 3-O-gentiobioside blocks the TGF-β/ALK5/Smad signaling pathway and inhibits epithelial-mesenchymal transition. It suppresses the proliferation, migration, invasion and metastatic growth of tumor cells. Kaempferol 3-O-gentiobioside alleviates airway inflammation and mucus hypersecretion in mice with allergic asthma. It reduces the volume of ovarian cancer xenografts in mice. Kaempferol 3-O-gentiobioside can be used in research related to allergic asthma, diabetes, MRSA infection, breast cancer, gastric cancer and ovarian cancer.
    Kaempferol 3-O-gentiobioside
  • 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-N1584C
    Halofuginone lactate
    Inhibitor 98.32%
    Halofuginone lactate, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone lactate is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone lactate is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone lactate has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
    Halofuginone lactate
  • HY-146434
    TGFβ-IN-2
    Inhibitor 99.37%
    TGFβ-IN-2 is an orally active TGF-β inhibitor. TGFβ-IN-2 suppresses the TGF-β-induced protein expression of COL1A1, α-SMA, and p-Smad3 in vitro. TGFβ-IN-2 demonstrates excellent anti-fibrotic efficacy in Bleomycin (HY-108345)-induced pulmonary fibrosis model. TGFβ-IN-2 can be used for the study of pulmonary fibrosis.
    TGFβ-IN-2
  • HY-P10414A
    Klotho-derived peptide 1 hydrochloride
    Inhibitor 99.67%
    Klotho-derived peptide 1 (KP1 human) hydrochloride 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 hydrochloride
  • HY-P990009
    Nisevokitug
    Inhibitor
    Nisevokitug (NIS-793) is a human, IgG2λ antibody targeting TGF-β (TGFB1/TGFB2). Nisevokitug is expressed by CHO-K1 cells.
    Nisevokitug
  • HY-B0252R
    Hydrochlorothiazide (Standard)
    Inhibitor
    Hydrochlorothiazide (Standard) is the analytical standard of Hydrochlorothiazide. This product is intended for research and analytical applications. 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 (Standard)
  • 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-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-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-P99720A
    Luspatercept (mIgG2a)
    Inhibitor 99.78%
    Luspatercept (mIgG2a) (RAP-536) is a fusion protein, consisting of a modified extracellular domain of human ActRIIB linked to the murine IgG2a Fc domain. Luspatercept (mIgG2a) inhibits Smad2/3 signaling, promotes differentiation of late-stage erythroid precursors and mitigates ineffective erythropoiesis (IE) in murine β-thalassemia. Luspatercept (mIgG2a) reduces anemia, α-globin aggregates, hemolysis, and disease complications of IE such as iron overload, splenomegaly, and bone defects.
    Luspatercept (mIgG2a)
  • HY-P10476
    Myostatin inhibitory peptide 2
    Inhibitor 99.75%
    Myostatin inhibitory peptide 2 (compd 2) is a myostatin inhibitor with a Kd of 35.9 nM. Myostatin inhibitory peptide 2 can be used for researches of muscle atrophic disorders.
    Myostatin inhibitory peptide 2
  • 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-W105318
    Pentabromophenol
    Inhibitor 99.94%
    Pentabromophenol (PBP) is a brominated flame retardant (BFR) widely used in various consumer products to reduce the flammability of materials used in different utility items. Pentabromophenol can accelerate the degradation of transforming growth factor-β (TGF-β) receptors by promoting clathrin-mediated endocytosis, thereby inhibiting the TGF-β signaling pathway. Additionally, Pentabromophenol can also induce apoptosis in peripheral blood mononuclear cells (PBMCs).
    Pentabromophenol
  • 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-B0252S
    Hydrochlorothiazid-d2
    Inhibitor 98.52%
    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-P991190
    Rilogrotug
    Inhibitor 99.9%
    Rilogrotug (AV-380) is a humanized IgG1 monoclonal antibody targeting GDF15.
    Rilogrotug
  • HY-N10303
    Withangulatin A
    Inhibitor 99.76%
    Withangulatin A is the inhibitor for COX-2. Withangulatin A inhibits MAPK, NF-κB, Akt/mTOR/p70S6K pathway, exhibits antitumor, anti-inflammatory and trypanocidal activities.
    Withangulatin A
  • HY-130687A
    Psicose
    Inhibitor 99.90%
    Psicose (DL-Psicose) is an orally effective sugar substitute. Psicose activates the PI3K/Akt/mTOR pathway to promote muscle synthesis. Psicose upregulates IGF-1 and downregulates Myostatin. Psicose normalizes mitochondrial dysfunction by increasing G6P activity. Psicose enhances the activity of antioxidant enzymes and reduces oxidative stress markers. Psicose increases muscle mass, grip strength and muscle weight in aged mice and diet-induced obese mice. Psicose improves obesity and type 2 diabetes. Psicose can be used in the research of age-related sarcopenia.
    Psicose
  • HY-B0252S2
    Hydrochlorothiazide-13C6
    99.61%
    Hydrochlorothiazide-13C6 is the 13C 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.
    Hydrochlorothiazide-<sup>13</sup>C<sub>6</sub>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity