TGF-beta/Smad Inhibitor

TGF-beta/Smad Inhibitors (114):

Cat. No.	Product Name	Effect	Purity

HY-159692

AZD8701	Inhibitor
AZD8701 (IONIS-1063734) is an antisense oligonucleotide targeting FOXP3 in regulatory T cells (Tregs). AZD8701 can relieve immunosuppression in cancer.

HY-N0158R

Oxymatrine (Standard)	Inhibitor
Oxymatrine (Standard) is the analytical standard of Oxymatrine. This product is intended for research and analytical applications. 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-117511

HJC0123	Inhibitor
HJC0123 is a STAT3 inhibitor. HJC0123 inhibits the proliferation of hepatic stellate cells and induces cell cycle arrest and apoptosis. HJC0123 reduces the phosphorylation, nuclear translocation and transcriptional activities of STAT3, increases the production of IL-6, inhibits the phosphorylation of Smad2/3 and down-regulates SOCS3. HJC0123 can be used in the study of liver fibrosis.

HY-170540

NOX4-IN-1	Inhibitor
NOX4-IN-1 (Compound 14m) is the inhibitor for NADPH oxidase 4 (NOX4), and blocks the generation of ROS. NOX4-IN-1 inhibits TGF-β1/Smad signaling pathway, decreases the expression of fibrosis-related proteins. NOX4-IN-1 inhibits the cell migration of NRK-49F.

HY-170813

P162-0948	Inhibitor
P162-0948 is a selective CDK8 inhibitor with an IC₅₀ value of 50.4 nM. P162-0948 reduces cell migration and protein expression of EMT-related proteins in A549 human alveolar epithelial cell lines. P162-0948 reduces phosphorylation of Smad, which suggests disruption of the TGF-β/Smad signaling pathway. P162-0948 is promising for research of pulmonary fibrosis.

HY-N2033R

Chebulinic acid (Standard)	Inhibitor
Chebulinic acid (Standard) is the analytical standard of Chebulinic acid. This product is intended for research and analytical applications. Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.

HY-N1584BR

Halofuginone (hydrochloride) (Standard)	Inhibitor
Halofuginone (hydrochloride) (Standard) is the analytical standard of Halofuginone (hydrochloride). 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[4].

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.

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.

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.

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.

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.

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.

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).

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.

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.

HY-P10476A

Myostatin inhibitory peptide 2 TFA	Inhibitor	99.12%
Myostatin inhibitory peptide 2 (compd 2) TFA is a myostatin inhibitor with a K_d of 35.9 nM. Myostatin inhibitory peptide 2 TFA can be used for researches of muscle atrophic disorders.

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.

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.

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.

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