TGF-beta/Smad Inhibitor

TGF-beta/Smad Inhibitors (136):

Cat. No.	Product Name	Effect	Purity

HY-B0673

Pirfenidone	Inhibitor	99.99%
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	99.62%
(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	99.28%
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-P991316

KD014	Inhibitor
KD014 (DX-2400) is a human monoclonal antibody (mAb) targeting MMP14 (K_i: 0.9 nM). KD014 inhibits TGFβ and SMAD2/3 activity, increases macrophage numbers and iNOS expression, and shifts macrophage phenotype toward anti-tumor M1-like. KD014 has anti-tumor activity in three different tumor models (MDA-MB-231, MDA-MB-435, and PC3). KD014 can be used in breast cancer research.

HY-P10359A

TAT-QFNP12 acetate	Inhibitor
TAT-QFNP12 acetate 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).

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	99.92%
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-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-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-P99100

Visugromab	Inhibitor	98.40%
Visugromab (CTL-002) is a GDF-15 neutralizing IgG4 mAb. Visugromab has synergistic anticancer activity with the anti-PD1 antibody Nivolumab (HY-P9903) and can effectively act on PD-1/PD-L1 relapsed/refractory metastatic solid tumors. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).

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 improves Bleomycin (HY-108345)-induced acute lung injury. 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-B0252

Hydrochlorothiazide	Inhibitor	99.46%
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-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-P99441

Apitegromab	Inhibitor	99.51%
Apitegromab (SRK-015) is an anti-promyostatin monoclonal antibody. Apitegromab can be used for the research of neuromuscular disease including spinal muscular atrophy.

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-160623

Rentosertib	Inhibitor	99.96%
Rentosertib (INS018 055) (compound 112) is the orally active TNIK and MAP4K4 inhibitor with IC₅₀ values of 12-120, 12-120 nM, respectively.

HY-12953

R-268712	Inhibitor	99.92%
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.

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