TGF-beta/Smad Inhibitor

TGF-beta/Smad Inhibitors (108):

Cat. No.	Product Name	Effect	Purity

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.

HY-115577

Mitochonic acid 35	Inhibitor
Mitochonic acid 35 is an IAA analogue with cytoprotective effects.

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 K_d of 29.7 nM. Myostatin inhibitory peptide 7 TFA can be used for researches of muscle atrophic disorders.

HY-120973

Butaprost free acid	Inhibitor
Butaprost free acid is a selective prostaglandin E receptor (EP2) agonist with an EC₅₀ of 33 nM and a K_i of 2.4 μM for murine EP2 receptor. Butaprost free acid is less activity against murine EP1, EP3 and EP4 receptors. Butaprost free acid attenuates fibrosis by hampering TGF-β/Smad2 signalling.

HY-P10899

ETTAC-2	Inhibitor	98.22%
ETTAC-2 is a LRG1 PROTAC degrader. ETTAC-2 promotes ubiquitination and degradation of LRG1 (DC₅₀ of 8.38 µM). ETTAC-2 inhibits the TGF-β-Smad3 signaling pathway and diminishes the secretion of fibrosis-associated proteins. ETTAC-2 attenuates the progression of renal fibrosis.

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.

HY-W707119

RepSox hydrochloride	Inhibitor
RepSox hydrochloride is a potent and selective inhibitor of transforming growth factor-β receptor I/activin-like kinase 5 (TGF-β-RI/ALK5). RepSox hydrochloride inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox hydrochloride can be used in the study of obesity and related metabolic diseases such as type 2 diabetes.

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