TGF-beta/Smad Activator

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

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.

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.

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. .

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).

AS2863619 is an orally active CDK8/19 inhibitor that also inhibits BMP2, MDA5 and RIG-I receptors. AS2863619 targets Stat5a-CDK8/19 to promote the differentiation of CD4⁺ T cells into regulatory T cells and induce FOXP3 expression, thereby restoring immune homeostasis and establishing transplant immune tolerance. AS2863619 also enhances the BMP2/SMAD signaling pathway to promote osteogenic differentiation and inhibit adipogenic differentiation. AS2863619 exerts osteoprotective effects by alleviating inflammation-induced impairment of osteogenic function and inducing neutrophil apoptosis (apoptosis). AS2863619 can be applied to research in related fields such as periodontitis-induced bone defects.

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.

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.

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

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.

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) .

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.

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.

AS2863619 free base is an orally active CDK8/19 inhibitor that also inhibits BMP2, MDA5 and RIG-I receptors. AS2863619 free base targets Stat5a-CDK8/19 to promote the differentiation of CD4⁺ T cells into regulatory T cells and induce FOXP3 expression, thereby restoring immune homeostasis and establishing transplant immune tolerance. AS2863619 free base also enhances the BMP2/SMAD signaling pathway to promote osteogenic differentiation and inhibit adipogenic differentiation. AS2863619 free base exerts osteoprotective effects by alleviating inflammation-induced impairment of osteogenic function and inducing neutrophil apoptosis (apoptosis). AS2863619 free base can be applied to research in related fields such as periodontitis-induced bone defects.

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.

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.

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. .

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.

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.

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.