TGF-beta/Smad Inhibitor

TGF-beta/Smad Inhibitors (108):

Cat. No.	Product Name	Effect	Purity

HY-B0673

Pirfenidone	Inhibitor	99.98%
Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities.

HY-13013

SIS3	Inhibitor	98.71%
(E)-SIS3 is a potent and selective inhibitor of Smad3 with an IC₅₀ of 3 μM for Smad3 phosphorylation. (E)-SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.

HY-N1584

Halofuginone	Inhibitor	99.92%
Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i 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.

HY-W005379

DGM	Inhibitor
DGM is an inhibitor of the TGF-β1/Smad signaling pathway with significant antifibrotic effects. DGM inhibits the epithelial-mesenchymal transition (EMT) process in alveolar epithelial cells and slows the progression of pulmonary fibrosis in vivo by reducing lung inflammation, improving lung function, and decreasing extracellular matrix (ECM) remodeling. DGM can be used in research on idiopathic pulmonary fibrosis (IPF) and EMT-related diseases.

HY-N1584C

Halofuginone lactate	Inhibitor	98.32%
Halofuginone lactate, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i 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.

HY-P10414A

Klotho-derived peptide 1 hydrochloride	Inhibitor
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.

HY-P99241

Ponsegromab	Inhibitor	99.41%
Ponsegromab (PF 06946860) is a potent and selective humanized anti-GDF15 monoclonal antibody with anti-cachexia activity. Ponsegromab binds to GDF15 and prevents the binding of GDF15 to GFRAL, thereby blocking GDF15/GFRAL-mediated signaling. Ponsegromab can be used in the research of cancers.

HY-N0158

Oxymatrine	Inhibitor	99.68%
Oxymatrine, an alkaloid from Sophora flavescens Alt. with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and TGF-β/Smad pathway. Oxymatrine inhibits bocavirus minute virus of canines (MVC) replication, reduces viral gene expression and decreases apoptosis induced by viral infection.

HY-P99720

Luspatercept	Inhibitor	98.92%
Luspatercept (ACE-536) is a recombinant modified ActRIIB fusion protein that binds with transforming growth factor β superfamily ligands. Luspatercept increases the erythrocyte numbers and promotes maturation of erythroid precursors. Luspatercept binds with GDF11 and inhibits Smad2/3 signaling. Luspatercept can be used for the research of anemia.

HY-100830

NCB-0846	Inhibitor	99.61%
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.

HY-N0587

Demethylzeylasteral	Inhibitor	99.92%
Demethylzeylasteral is an orally active triterpenoid compound isolated from Tripterygium wilfordii, which has functions such as anti-inflammatory, anti-tumor, anti fertility, estrogen metabolism regulation, immune suppression, and immune system regulation ^[1][2].

HY-N1584A

Halofuginone hydrobromide	Inhibitor	99.99%
Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i 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.

HY-101275

EMT inhibitor-1	Inhibitor	99.45%
EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.

HY-P0118B

Disitertide diammonium	Inhibitor	99.53%
Disitertide (P144) diammonium is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide diammonium is also a PI3K inhibitor and an apoptosis inducer.

HY-P99020

Fresolimumab	Inhibitor	99.51%
Fresolimumab (GC1008) is a human monoclonal antibody against TGF-β that neutralizes all mammalian active subtypes of TGF-β. The binding affinity of Fresolimumab to TGF-β2 is 1.8 nM. Fresolimumab radiolabeled with ⁸⁹Zr can be used for PET analysis of TGF-β expression, antibody uptake and organ distribution. Fresolimumab can be used in the study of cancer, osteogenesis imperfecta, fibrosis and kidney disease.

HY-12953

R-268712	Inhibitor	99.88%
R-268712 is an orally active and selective ALK-5 inhibitor, with an IC₅₀ of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC₅₀ of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer.

HY-W012977

3,3-Dimethyl-1-butanol	Inhibitor	99.56%
3,3-Dimethyl-1-butanol (DMB) is an orally active inhibitor of trimethylamine (TMA) and trimethylamine N-oxide (TMAO). 3,3-Dimethyl-1-butanol inhibits the signaling pathway of p65 NF-κB and TGF-β1/Smad3. 3,3-Dimethyl-1-butanol has potential applications in cardiovascular disease (CVD).

HY-B0252

Hydrochlorothiazide	Inhibitor	99.51%
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.

HY-P99388

Trevogrumab	Inhibitor	98.86%
Trevogrumab (REGN-1033) is a monoclonal antibody targeting GDF8 (growth differentiation factor 8, also known as myostatin). Trevogrumab is used in research on muscle wasting conditions, including disuse atrophy, chronic diseases, and changes in food and nutrient intake.

HY-150795

SY-LB-35	Inhibitor	≥98.0%
SY-LB-35 is a potent bone morphogenetic protein (BMP) receptor agonist. SY-LB-35 can stimulate significant increases in cell number and cell viability in the C2C12 myoblast cell line, and causes shifts towards the S and G2/M phases of the cell cycle. SY-LB-35 stimulates canonical Smad and non-canonical PI3K/Akt, ERK, p38 and JNK intracellular signaling pathways.

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