Catalog No.
Product Name
Application
Product Information
Citations
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Smad2/3 Inhibitor
Luspatercept is a recombinant modified ActRIIB fusion protein that functions as a Smad2/3 inhibitor. It selectively binds to transforming growth factor β (TGF-β) superfamily ligands, including GDF11, thereby inhibiting Smad2/3 signaling. This compound promotes the maturation of erythroid precursors and increases erythrocyte numbers, making it a valuable tool for research into anemia and related erythropoietic disorders. -
SMAD7 Antisense Oligonucleotide
Mongersen sodium is a targeted SMAD7 antisense oligonucleotide that functions to restore TGF-β1 activity, resulting in the inhibition of inflammatory signaling pathways. This compound has demonstrated efficacy in attenuating experimental colitis resembling Crohn's disease in mouse models. It is a valuable tool for studying inflammatory bowel disease mechanisms and the modulation of TGF-β signaling in various research applications. -
Smad3 Inhibitor
SIS3 free base is a potent and selective inhibitor of Smad3 phosphorylation. It significantly inhibits the myofibroblast differentiation of fibroblasts induced by TGF-β1 while leaving the phosphorylation of Smad2 unaffected. This specificity makes SIS3 free base a valuable tool for studying the role of Smad3 in cellular processes associated with fibrosis and other TGF-β1 mediated pathways. -
Syk Inhibitor, NF-κB p65 Inhibitor, TGF-β1/Smad Signaling Inhibitor
Flavanomarein is a potent inhibitor of Syk and NF-κB p65, as well as a modulator of TGF-β1/Smad signaling pathways. This compound exhibits cytoprotective, anti-inflammatory, and antioxidant activities, enhancing AKT phosphorylation while regulating key proteins such as PKC-δ, P85α, PKC-β1, Sirt1, Bcl-2, and ICAD. Flavanomarein also inhibits the nuclear translocation of NF-κB p65 and modulates epithelial-mesenchymal transition (EMT) markers, promoting proliferation in HK-2 cells and protecting neuronal cells from 6-OHDA-induced neurotoxicity. This compound is valuable for research on Parkinson's disease and diabetic nephropathy. -
TGF-β2 Antisense Aligonucleotide
Trabedersen is an antisense oligodeoxynucleotide that specifically targets and inhibits TGF-β2, a key regulator in the TGF-beta/Smad signaling pathway. This reagent is critical for research in malignant brain tumors and various solid tumors, including those affecting the skin, pancreas, and colon, which exhibit overexpression of TGF-β2. By modulating this pathway, Trabedersen offers insights into tumor biology and potential therapeutic strategies. -
TGF-β Inhibitor
TGFβ-IN-2 is an orally active inhibitor of TGF-β, targeting its signaling pathways. This compound effectively suppresses TGF-β-induced expression of key proteins such as COL1A1, α-SMA, and p-Smad3 in vitro. TGFβ-IN-2 exhibits significant anti-fibrotic effects in a Bleomycin-induced pulmonary fibrosis model, making it a valuable tool for investigating the mechanisms and potential treatments of pulmonary fibrosis. -
SMAD7 Antisense Oligonucleotide
Mongersen is a targeted SMAD7 antisense oligonucleotide that restores TGF-β1 activity, thereby inhibiting inflammatory pathways. This compound has demonstrated the ability to attenuate experimental colitis resembling Crohn's disease in murine models. Its application is particularly relevant in studying inflammation and fibrosis related to gastrointestinal disorders. -
TGF-β1/Smad Signaling Pathway Inhibitor
DGM is a specific inhibitor of the TGF-β1/Smad signaling pathway, exhibiting notable antifibrotic properties. It effectively inhibits the epithelial-mesenchymal transition (EMT) in alveolar epithelial cells, thereby slowing the progression of pulmonary fibrosis in vivo. DGM reduces lung inflammation, enhances lung function, and minimizes extracellular matrix remodeling, making it a valuable tool for research on idiopathic pulmonary fibrosis (IPF) and other EMT-related diseases. -
TGF-β1 Inhibitory Peptide
P17 Peptide is a selective inhibitor of human TGF-β1, functioning by blocking its activity. This peptide is valuable for studying the role of TGF-β1 in various biological processes and disease states, including fibrosis and cancer. Its inhibitory effects facilitate research into therapeutic strategies targeting TGF-β signaling pathways. -
TGF-β1 Inhibitor
DT-6 is a selective inhibitor of TGF-β1, a key regulator of cellular processes related to fibrosis and cancer progression. By inhibiting TGF-β1, DT-6 effectively disrupts M2 macrophage-induced epithelial to mesenchymal transition (EMT) and inhibits the invasive migration of cancer cells. This compound is valuable for research applications focused on cancer biology and related therapeutic interventions. -
TGF-β2 siRNA
ISTH0036 is a selective antisense oligonucleotide targeting transforming growth factor beta 2 (TGF-β2). It exhibits inhibitory activity against TGF-β2 expression, making it a valuable tool for investigating the pathophysiological mechanisms of primary open-angle glaucoma (POAG) and wet age-related macular degeneration. This reagent is suitable for both in vitro and in vivo studies aimed at understanding the role of TGF-β2 in these ocular conditions. -
SMAD2 activator
Myristoyl tetrapeptide-12 is a specific activator of SMAD2, promoting the recruitment of SMAD3 to DNA. This peptide exhibits significant biological activity in stimulating hair growth, with notable effects on eyelash enhancement. Its applications are particularly relevant in research focusing on hair follicle biology and regenerative medicine. -
TGF-β/Smad/MAPK Inhibitor
TGF-β/Smad-IN-3 is a potent inhibitor of the TGF-β/Smad signaling pathway and MAPK pathway. This compound demonstrates significant anti-pulmonary fibrosis activity by inhibiting collagen deposition resulting from TGF-β1, with an IC50 of 3.21 μM. Additionally, TGF-β/Smad-IN-3 effectively reduces the expression of α-SMA, COL1A1, and FN in TGF-β1-induced CCC-HPF-1 cells, while also significantly reducing cell migration. This reagent is valuable for research focused on pulmonary fibrosis and related fibrosis-related mechanisms. -
TGF-β1/Smad Inhbitor
TGF-β1/Smad-IN-1 is a potent inhibitor of the TGF-β1/Smad signaling pathway, which plays a crucial role in the regulation of fibrotic processes. This compound effectively reduces the expression of fibrosis markers, such as α-SMA and COL1A1, induced by TGF-β1, demonstrating significant antifibrotic activity. TGF-β1/Smad-IN-1 is valuable for research applications focused on hepatic fibrosis and related fibrotic disorders. -
TGF-β1 Inhibitor
H-Leu-Ser-Lys-Leu-OH (LSYL) is an inhibitor of TGF-β1 activation, functioning as a latency-associated peptide derived from the amino terminus of LAP. By binding to KRFK, it effectively obstructs the signaling pathway of TGF-β1, thereby mitigating hepatic damage and fibrosis. This compound serves as a valuable tool for research into therapeutic interventions targeting TGF-β1-mediated pathways in fibrotic diseases. -
TGF-β1 Inhibitor
PXS 64 is a selective inhibitor of TGF-β1, targeting the activation of latent transforming growth factor-beta 1. This lipophilic prodrug, a mannose-6-phosphate analogue, demonstrates potent anti-fibrotic activity by attenuating the TGF-β1 signaling pathway in human lung fibroblasts. It effectively reduces the expression of key fibrotic markers including collagen IV, fibronectin, MCP-1, and phospho-Smad2 in renal cells. PXS 64 is applicable in research related to chronic kidney disease, idiopathic pulmonary fibrosis, and dermal scarring, making it a valuable tool for studies of fibrotic disorders. -
Myo1s/TGF-β Inhibitor
Pentachloropseudilin is a potent reversible allosteric inhibitor targeting Myo1s (class 1 myosins), exhibiting IC50 values ranging from 1 to 5 μM for mammalian class-1 myosins, while displaying greater than 90 μM for class-2 and class-5 myosins. Additionally, it effectively inhibits transforming growth factor-β (TGF-β) signaling, with an IC50 of 0.1 to 0.2 μM. This compound is valuable for research in cellular signaling pathways and myosin function, contributing to studies in cell motility and tissue remodeling. -
Anti-CD73/TGF-β Antibody
Dalutrafusp alfa is a bifunctional antibody that targets CD73 and TGF-β, key components involved in the immunosuppressive pathway. This compound modulates immune responses by inhibiting adenosine production and blocking TGF-β signaling. It is primarily utilized in research focused on tumor immunology and the modulation of immune checkpoints. Its unique mechanism allows for exploration in various therapeutic applications, particularly in cancer treatment and autoimmune diseases. -
ALK4/5/7 Inhibitor
A 83-01 sodium is a selective inhibitor of the transforming growth factor-beta (TGF-β) type I receptors ALK4, ALK5, and ALK7. With IC50 values of 12 nM, 45 nM, and 7.5 nM, it effectively blocks transcriptional activity induced by these kinases. This compound is valuable for research applications focused on TGF-β signaling pathways and regulation of cellular processes such as proliferation, differentiation, and epithelial-mesenchymal transition. -
ACVR2A-IgG Fc Fusion Protein
Sotatercept is a soluble activin receptor 2A (ACVR2A) IgG Fc fusion protein that modulates growth differentiation pathways by combining activin and growth differentiation factor signals. This compound has demonstrated potential biological activity in restoring the balance between growth promotion and inhibition, making it a promising candidate for research in pulmonary arterial hypertension, anemia, bone loss, erythropoiesis, and osteolytic lesions associated with multiple myeloma. Its function highlights its value in studying conditions related to dysregulated signaling pathways in these diseases. -
TGFbR1 Inhibitor
PF-06952229 is a potent and selective inhibitor of TGFbR1, demonstrating oral bioavailability. By specifically binding to TGFbR1, it effectively blocks TGFbR1-mediated signaling pathways. This compound shows significant promise as an antineoplastic agent, particularly in the study of solid tumors, including metastatic breast cancer. Its mechanism makes it a valuable tool for understanding TGFbR1's role in cancer progression and therapy. -
TGFβ1 Inhibitor
TGFβ1-IN-1 is a potent inhibitor of transforming growth factor-beta 1 (TGF-β1). This compound effectively inhibits the upregulation of fibrosis markers such as α-SMA and fibronectin, making it a valuable tool for investigating liver fibrosis and related pathologies. TGFβ1-IN-1 is suitable for research applications focused on fibrosis modulation and therapeutic interventions targeting TGF-β1 signaling pathways. -
BMPR2 Inhibitor
CDD-1653 is a potent and selective inhibitor of Bone Morphogenetic Protein Receptor 2 (BMPR2) with an IC50 of 2.8 nM. By diminishing ATP binding to the kinase domain of BMPR2, CDD-1653 modulates the phosphorylation of SMAD1/5/8 transcription factors, which are essential components of the BMP signaling pathway. This reagent is suitable for investigating diseases associated with dysregulation in the BMP signaling cascade. -
ALK5 Inhibitor
Vactosertib Hydrochloride is a potent inhibitor of activin receptor-like kinase 5 (ALK5), characterized by its ATP-competitive mechanism and an IC50 of 12.9 nM. Additionally, it demonstrates inhibitory effects on ALK2 and ALK4 with IC50 values of 17.3 nM. This compound exhibits significant antimetastatic activity and anticancer properties, making it a valuable research tool for studies related to cancer biology and therapeutic development targeting TGF-β signaling pathways. -
Bifunctional Fusion Protein
Bintrafusp alfa is a bifunctional fusion protein that consists of the extracellular domain of TGF-β receptor II fused to a human IgG1 monoclonal antibody, which inhibits programmed cell death ligand. This innovative reagent exhibits significant anti-tumor activity by modulating immune responses and transforming the tumor microenvironment. Bintrafusp alfa is primarily utilized in cancer research to explore its therapeutic potential and enhance understanding of immune evasion mechanisms in tumors. -
ALK5 Inhibitor
THRX-144644 is a selective ALK5 inhibitor with a very low IC50 value of 0.14 nM, demonstrating potent inhibition of the TGFβ signaling pathway. This compound is designed for lung-targeted applications, offering an alternative that minimizes systemic toxicities typically linked to broader TGFβ pathway inhibition. THRX-144644 is valuable for research projects focused on fibrosis, cancer biology, and respiratory diseases. -
TGF-β Inhibitor
Pentabromopseudilin (PBrP) is a potent inhibitor of transforming growth factor-β (TGF-β), functioning as a reversible allosteric modulator of myosin Va (MyoVa). Isolated from marine bacteria, PBrP displays significant antimicrobial, anti-tumor, and phytotoxic properties. This compound is valuable for research in fibrotic diseases and cancer, providing insight into TGF-β mediated pathways and their implications in disease progression. -
BMP Receptor Agonist
SY-LB-57 is a potent agonist of bone morphogenetic protein (BMP) receptors, facilitating BMP signaling pathways. This compound demonstrates significant biological activity in promoting bone formation and has potential applications in research related to osteogenesis, fracture healing, and pulmonary arterial hypertension. Its ability to enhance BMP signaling makes SY-LB-57 a valuable tool in the study of skeletal and vascular diseases. -
ALK5 Inhibitor
IN-1130 is a highly selective inhibitor of the transforming growth factor-β type I receptor kinase (ALK5), exhibiting an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. This compound also demonstrates inhibitory effects on ALK5 phosphorylation of casein with an IC50 of 36 nM and on p38α mitogen-activated protein kinase at an IC50 of 4.3 μM. IN-1130 is beneficial for research focused on renal fibrosis in obstructive nephropathy as well as the blockage of breast cancer lung metastasis, providing valuable insights into TGF-β signaling pathways. -
TGF-β Inhibitor
CJJ300 is a selective inhibitor of transforming growth factor-β (TGF-β), exhibiting an IC50 value of 5.3 µM. It effectively disrupts the formation of the TGF-β-TβR-I-TβR-II signaling complex, thereby inhibiting TGF-β signaling pathways. This compound is valuable for research applications focused on the modulation of TGF-β related processes, including fibrosis, cancer progression, and immune regulation. -
ALK5 Inhibitor
ALK5-IN-8 is a potent inhibitor of transforming growth factor beta receptor I (TGFβRI, also known as ALK5). This compound effectively blocks the phosphorylation of downstream signaling proteins such as Smad2 and Smad3 by preventing the binding of TGFβRI to its ligands, thereby disrupting TGF-β signaling pathways. ALK5-IN-8 is valuable for research into various diseases associated with ALK5-mediated signaling, contributing to the understanding of pathophysiological conditions influenced by TGF-β. -
ALK5 Inhibitor
Ontunisertib is a selective inhibitor of ALK5 (TGFβR1) that exhibits oral bioavailability and gastrointestinal restriction. By inhibiting the TGFβ signaling pathway, Ontunisertib effectively interferes with pro-fibrotic processes. This compound is primarily utilized in research focused on fibrostenotic Crohn’s disease, providing insights into its pathophysiology and potential therapeutic strategies. -
TGF beta-1 Inhibitor
Vicatertide is an inhibitor of TGF-beta-1 (transforming growth factor beta 1), a key regulator in cellular signaling pathways associated with fibrosis and immune responses. By modulating TGF-beta-1 activity, Vicatertide demonstrates potential in research applications focused on fibrotic diseases, cancer progression, and tissue repair mechanisms. Its use contributes to a deeper understanding of TGF-beta-related pathways in various biological contexts. -
ALK2 Inhibitor
Zilurgisertib is a selective ALK2 inhibitor that exhibits an IC50 value of 15 nM. This compound effectively inhibits the phosphorylation of SMAD1/5, demonstrating an IC50 of 63 nM. Zilurgisertib has been shown to reduce hepcidin production, making it a potential therapeutic agent for the management of anemia. This reagent is particularly relevant for research applications in melanoma studies. -
TGFBR1 Inhibitor
AZ12799734 is a selective TGFBR1 kinase inhibitor with an IC50 of 47 nM. This compound functions as a pan inhibitor of BMP and TGFβ signaling pathways, making it a valuable tool for research in fibrosis, oncology, and other areas of disease where TGFβ and BMP signaling are implicated. Its oral bioavailability enhances its applicability in preclinical studies and potential therapeutic development. -
Selective TGFBR1 Inhibitor
AZ12601011 is a selective inhibitor of TGFBR1, exhibiting an IC50 of 18 nM and a Kd of 2.9 nM. This compound effectively inhibits the phosphorylation of SMAD2 by targeting ALK4, TGFBR1, and ALK7, thereby modulating TGF-β signaling pathways. AZ12601011 demonstrates anti-tumor activity, particularly in inhibiting mammary tumor growth, making it a valuable tool for research in cancer biology and therapeutic development. -
TGFβ Inhibitor
TGFβ-IN-5 is a selective inhibitor of TGF-β signaling, providing a valuable tool for investigating fibroproliferative diseases linked to this pathway. By modulating TGF-β activity, TGFβ-IN-5 may contribute to a better understanding of pathological tissue remodeling and fibrosis. This compound is essential for research in areas such as cancer, wound healing, and chronic inflammatory conditions. -
TGFβR1 Inhibitor
BMS-986260 is a selective and orally bioavailable inhibitor of TGFβR1, exhibiting a potent inhibitory capacity with an IC50 of 1.6 nM. It demonstrates remarkable selectivity for TGFβR1 over TGFβR2 and remains effective across a broad spectrum of over 200 kinases. BMS-986260 effectively inhibits TGFβ-mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cell lines, with IC50 values of 350 nM and 190 nM, respectively. It serves as a valuable tool for research in immuno-oncology and fibrosis. -
ALK5 Inhibitor
TP-008 is a selective and orally active inhibitor of Activin-Like Kinase 5 (ALK5) with potent biological activity, demonstrating pIC50 and pEC50 values of 7.6 and 6.63, respectively. This compound serves as a valuable tool for investigating the role of ALK5 in TGF-β signaling and its implications in fibrosis and other pathophysiological conditions. Caution is warranted, as high doses have been associated with observed cardiac toxicity in vivo. -
TGFβR1 Inhibitor
TGFβRI-IN-3 is a selective inhibitor of TGFβR1, exhibiting an IC50 of 0.79 nM and demonstrating 2000-fold selectivity against MAP4K4. This compound effectively modulates TGFβ signaling pathways, making it a valuable tool for research in immuno-oncology. Its specificity and potency position TGFβRI-IN-3 as a promising candidate for further investigations into the therapeutic targeting of TGFβR1 in cancer treatments. -
ALK5 Inhibitor
GW-6604 is an inhibitor of ALK5, exhibiting an IC50 value of 140 nM for autophosphorylation inhibition. This compound serves as a valuable tool for investigating the molecular mechanisms associated with liver fibrosis. Its selective inhibition of ALK5 makes it relevant for research studies focused on fibrotic disease pathways and potential therapeutic interventions. -
TGF-βRI Inhibitor
GFH018 is a selective inhibitor of TGF-β receptor I (TGF-βRI), targeting the signaling pathways associated with cellular proliferation and differentiation. This compound demonstrates significant potential in modulating TGF-β signaling, making it a valuable tool for studying its role in cancer progression and fibrosis. GFH018 is suitable for applications in cancer research, particularly in investigating therapeutic strategies that disrupt TGF-β-mediated tumor microenvironments. -
TGF-β Receptor Inhibitor
HYL001 is a potent inhibitor of the TGF-β receptor 1 (ALK5). This compound demonstrates approximately nine times greater potency compared to structurally related inhibitors. HYL001 effectively reduces liver metastases in murine models, making it a valuable tool for research in cancer biology and therapeutic development targeting TGF-β signaling pathways. -
BMP Agonist
BMP Agonist 2 is a potent bone morphogenetic protein (BMP) agonist that enhances bone tissue generation by increasing osteoblast activity and proliferation. It acts primarily through the BMP2-ATF4 signaling pathway, facilitating the differentiation of osteoblasts critical for bone formation. This reagent is valuable for research applications related to senile osteoporosis and other conditions involving bone density and regeneration. -
ALK2 Inhibitor
KER047 is a potent inhibitor of activin receptor-like kinase-2 (ALK2). This compound is primarily utilized in research focused on metabolic diseases, particularly fibrodysplasia ossificans progressiva (FOP). KER047's ability to target ALK2 makes it a valuable tool for investigating the molecular mechanisms underlying these conditions. -
ALK2 Inhibitor
KER047 succinate is a potent inhibitor of activin receptor-like kinase 2 (ALK2). This compound demonstrates significant inhibition of ALK2 activity, making it a valuable tool for investigating metabolic diseases, particularly fibrodysplasia ossificans progressiva (FOP). Research applications of KER047 succinate include studies focused on the modulation of bone formation and the exploration of therapeutic strategies for disorders related to aberrant bone growth. -
ACVR2 Antagonist
Ramatercept is a soluble activin receptor 2 (ACVR2) antagonist that functions by inhibiting the signaling pathway associated with muscle growth suppression. It has demonstrated potential in the treatment of muscle atrophy by modulating myostatin activity, making it a valuable tool for research in muscle biology and related therapeutic applications. Researchers may utilize Ramatercept to explore mechanisms of muscle wasting and to develop strategies for promoting muscle growth. -
ALK2 Inhibitor
M4K2163 dihydrochloride is a selective inhibitor of activin receptor-like kinase-2 (ALK2) with a blood-brain barrier (BBB) permeability, exhibiting an IC50 value of 19 nM. This compound is valuable for research focused on diffuse intrinsic pontine glioma (DIPG), providing a tool for elucidating the role of ALK2 in various biological processes and potential therapeutic strategies. -
BMP Potentiator
Chromenone 1 is a potent enhancer of bone morphogenetic protein (BMP) signaling. It uniquely activates a pronounced, kinase-independent negative feedback mechanism on TGFβ, leading to an amplification of BMP-Smad signaling pathways within the nucleus. This compound is valuable for research into osteogenic differentiation and bone regeneration. -
TGF-β Receptor Inhibitor
TGFβR-IN-1 is a potent inhibitor of the transforming growth factor-beta receptor (TGF-βR), designed for selective activation in tumor environments. This compound exhibits significant biological activity by blocking TGF-β signaling pathways, which are often implicated in tumor progression and immune evasion. TGFβR-IN-1 is suitable for research applications focused on cancer biology, fibrosis, and the modulation of immune responses.
