TGF-beta/Smad Activator

TGF-beta/Smad Activators (34):

Cat. No.	Product Name	Effect	Purity

HY-183067A

TAS1440 benzoate	Activator
TAS1440 benzoate is an orally active LSD1/KDM1A inhibitor with a human IC₅₀ of 4.8 nM. TAS1440 benzoate non-covalently binds to the histone H3-binding pocket of LSD1, inhibiting demethylase activity and disrupting repressive complexes with INSM1 and SMAD2. TAS1440 benzoate activates tumor-suppressive TGF-β and NOTCH signaling pathways via transcriptional reprogramming. TAS1440 benzoate can be used for the research of small cell lung cancer, specifically the SCLC-A subtype.

HY-16268

Kartogenin	Activator	99.05%
Kartogenin (KGN) is an inducer of chondrogenic tissue formation (EC₅₀: 100 nM). Kartogenin induces chondrogenesis by binding to fibrin A, disrupting its interaction with the transcription factor core binding factor beta subunit (CBFβ), and by modulating the CBFβ-RUNX1 transcriptional program. Kartogenin also promotes tendon-bone junction (TBJ) wound healing by stimulating collagen synthesis. Kartogenin is widely used in cell-free therapy in the field of regeneration for cartilage regeneration and protection, tendon-bone healing, wound healing and limb development. Kartogenin promotes cartilage repair, coordinates limb development, and is also used in osteoarthritis (OA) research.

HY-116084

Trimethylamine N-oxide	Activator	98.0%
Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.

HY-W016562

Hippuric acid	Activator	99.98%
Hippuric Acid is an orally active metabolite. Hippuric Acid can be produced by intestinal microorganisms from the metabolism of polyphenols, benzoic acid. Hippuric Acid decreases NRF2, MMP9 and leads to ROS accumulation. Hippuric Acid activates TGFβ/SMAD signaling. Hippuric Acid improves hyperuricemia and colitis. Hippuric Acid can also be used in cardiovascular disease research. .

HY-112499

Menaquinone-7	Activator	98.51%
Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs (orally active), is originally discovered as the anti-hemorrhagic factors. Menaquinone-7 inhibits osteoclast bone resorption in vitro and stimulates bone formation in femoral tissue of aged female rats. Menaquinone-7 has a well-researched potential in the prevention of aging-induced bone degeneration. Menaquinone-7 is also a pharmacological option for activating Gla matrix protein and intervening in the progression of calcific aortic stenosis (CAVS).

HY-N0038

Alantolactone	Activator	99.94%
Alantolactone is a selective STAT3 inhibitor, with potent anticancer activity. Alantolactone induces apoptosis in cancer.

HY-108915

Trimethylamine N-oxide dihydrate	Activator	99.86%
Trimethylamine N-oxide dihydrate is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide dihydrate induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide dihydrate also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.

HY-116084S

Trimethylamine N-oxide-d₉	Activator	99.76%
Trimethylamine N-oxide-d₉ is the deuterium labeled Trimethylamine N-oxide. Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.

HY-N1499

Nystose	Activator	99.98%
Nystose is a tetrasaccharide with two fructose molecules linked via beta (1→2) bonds to the fructosyl moiety of sucrose. Nystose exhibits prebiotic, immunomodulatory, and metabolism regulating activities. Nystose promotes the bone mineralization by activating the Wnt/β-catenin signaling pathway.

HY-W011121

2-Oleoylglycerol	Activator	99.9%
2-Oleoylglycerol (2-OG) is a lipid found in the diet. It is a GPR119 agonist, with an EC₅₀ value of 2.5 μM in activating hGPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol enhances the inflammatory response of macrophages and promotes fibrosis by activating the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. It also stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. 2-Oleoylglycerol is expected to be used in the research of non-alcoholic steatohepatitis (NASH) .

HY-119575

Tetramethyluric acid	Activator	99.63%
Tetramethyluric acid (1,3,7,9-Tetramethyluric acid) is an orally active purine alkaloid in Coffea species and Camellia kucha. Tetramethyluric acid exhibits antiviral, and anti-inflammatory activity. Tetramethyluric acid can be used for the research of inflammation disease, and influenza virus infection.

HY-147372

SJ000063181	Activator	98.92%
SJ000063181 is a potent BMP signaling activator. SJ000063181 activates BMP4 and the phosphorylation of SMAD1/5/8 (p-SMAD1/5/8). SJ000063181 induces ventralization in zebrafish embryos.

HY-P5832

BMP2-derived peptide	Activator	98.04%
BMP2-derived peptide is an osteogenic inducer and BMP receptor ligand. BMP2-derived peptide binds to BMP receptors on the cell surface to form a complex, activates the downstream Smad signaling pathway, and regulates the expression of osteogenic transcription factors. BMP2-derived peptide effectively promotes the adhesion, proliferation, osteogenic differentiation and mineralization of bone marrow mesenchymal stem cells, significantly up-regulates the mRNA levels of OCN, Runx2 and type I collagen, and increases alkaline phosphatase activity and calcium deposition. BMP2-derived peptide induces osteoblast differentiation and ectopic bone regeneration, and improves cranial bone defect repair. Meanwhile, BMP2-derived peptide enhances the cytocompatibility of mesoporous silica nanoparticles, synergistically increases osteogenic activity with Dexamethasone (HY-14648), serving as an important tool for bone defect repair research.

HY-W014841

Sodium hippurate, 98%	Activator	99.91%
Sodium hippurate, 98% is an orally active metabolite. Sodium hippurate, 98% can be produced by intestinal microorganisms from the metabolism of polyphenols, benzoic acid. Sodium hippurate, 98% decreases NRF2, MMP9 and leads to ROS accumulation. Sodium hippurate, 98% activates TGFβ/SMAD signaling. Sodium hippurate, 98% improves hyperuricemia and colitis. Sodium hippurate, 98% can also be used in cardiovascular disease research. .

HY-N2013

Aristolactam I	Activator	99.44%
Aristolactam I is an AQP1 inhibitor and Aristolochic acid I metabolite. Aristolactam I can be isolated from Aristolochia plants. Aristolactam I downregulates Twist1 expression, increases E-cadherin expression, and activates the TGF-β/Smad signaling pathway. Aristolactam I has anticancer activity against breast cancer. Aristolactam I is nephrotoxic. Aristolactam I is mainly used in the study of breast cancer and kidney diseases such as renal interstitial fibrosis.

HY-112247

SR 16832	Activator	99.58%
SR 16832 is a dual-site covalent, orthosteric and allosteric PPARγ antagonist. SR 16832 activates the TGF-β signaling pathway and upregulates the expression of Vimentin and Fibronectin (Fibronectin). SR 16832 is toxic to bronchial epithelium. SR 16832 can be used in research related to type 2 diabetes and pulmonary fibrosis.

HY-16268A

Kartogenin sodium	Activator	99.84%
Kartogenin (KGN) sodium is an inducer of chondrogenic tissue formation (EC₅₀: 100 nM). Kartogenin sodium induces chondrogenesis by binding to fibrin A, disrupting its interaction with the transcription factor core binding factor beta subunit (CBFβ), and by modulating the CBFβ-RUNX1 transcriptional program. Kartogenin sodium also promotes tendon-bone junction (TBJ) wound healing by stimulating collagen synthesis. Kartogenin sodium is widely used in cell-free therapy in the field of regeneration for cartilage regeneration and protection, tendon-bone healing, wound healing and limb development. Kartogenin sodium promotes cartilage repair, coordinates limb development, and is also used in osteoarthritis (OA) research.

HY-N0363

(+)-Columbianetin	Activator	99.04%
(+)-Columbianetin ((S)-Columbianetin) acts as an inhibitor of JNK/ERK. (+)-Columbianetin inhibits UVA-induced phosphorylation of JNK and ERK, reduces the production of MMP-1, reverses UVA-induced Collagen (HY-NP003) degradation, and alleviates UVA-mediated inhibition of Smad2/3 phosphorylation and translocation. (+)-Columbianetin regulates the AP-1 and ASK1-MAPK signaling pathways, inhibits the production of ROS and blocks sub-G₁ cell cycle arrest. (+)-Columbianetin is applicable to research related to skin aging.

HY-W142432

Perfluoroundecanoic acid	Activator	99.85%
Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation.

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.

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