Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Anti-BMP-6 Antibody
Bezeotermin alfa is an anti-BMP-6 antibody designed to selectively target and inhibit bone morphogenetic protein 6 (BMP-6). This recombinant fusion protein plays a significant role in modulating BMP signaling pathways, which are crucial for bone development and homeostasis. Bezeotermin alfa is primarily used in research focused on understanding bone diseases, tissue engineering, and regenerative medicine applications. -
TGFβRI Inhibitor
Galunisertib monohydrate is a selective inhibitor of the TGF-β receptor type I (TGF-βRI), exhibiting an IC50 of 56 nM. This compound effectively modulates TGF-β signaling pathways, which are implicated in various fibrosis and cancer progression contexts. Galunisertib is utilized in research applications focusing on therapeutic strategies targeting TGF-βRI to mitigate tumor microenvironment effects and promote antitumor immunity. -
TGFβRI Inhibitor
TGFβRI-IN-6 is a highly effective inhibitor of TGFβ receptor I, demonstrating an IC50 of 0.55 nM. This compound has shown promise in enhancing anti-tumor immunity, making it a valuable tool for cancer research. Its specific targeting of TGFβRI allows for detailed investigation into the modulation of immune responses in the tumor microenvironment. -
ALK5 Inhibitor
ALK5-IN-10 is a selective inhibitor of the TGF-β type I receptor kinase ALK5, exhibiting IC50 values of 0.007 μM for ALK5 and 1.98 μM for p38α. This compound demonstrates significant potential in modulating the TGF-β signaling pathway, making it a valuable tool for cancer research and therapeutic development. Its specificity for ALK5 allows for targeted investigations into tumorigenesis and associated pathways. -
ALK-5 Inhibitor
ALK-5-IN-1 is a selective inhibitor of ALK-5 (activin receptor-like kinase 5), a critical receptor in the TGF-beta signaling pathway. This compound demonstrates significant anti-fibrotic and anti-cancer activity, making it a valuable tool in preclinical studies investigating fibrosis-related conditions and tumor progression. It is suitable for researchers exploring the roles of TGF-beta signaling in diverse biological processes and therapeutic strategies. -
ALK5 Inhibitor
ALK5-IN-9 is a potent inhibitor of TGFβRI (ALK5) that effectively disrupts autophosphorylation of the kinase. With an IC50 of 25 nM for ALK5 and 74.6 nM for NIH3T3 cell activity, this compound demonstrates significant biological efficacy. ALK5-IN-9 exhibits a favorable pharmacokinetic profile and reduced hERG inhibition, making it a valuable tool for investigating the role of TGFβ signaling in various cancer research applications. -
TGF-βRI Inhibitor
GFH018 methylbenzenesulfonate is a selective inhibitor of TGF-β receptor I (TGF-βRI), a key regulator in the TGF-β signaling pathway. By inhibiting TGF-βRI, GFH018 effectively modulates cellular processes related to cancer progression and fibrosis. This reagent is particularly valuable for research applications focused on tumor microenvironment interactions, epithelial-mesenchymal transition, and therapeutic interventions in oncological studies. -
ALK-5 Inhibitor
ALK5-IN-33 is a selective inhibitor of ALK-5, exhibiting an IC50 of 10 nM or lower. This compound effectively interferes with the ALK-5 signaling pathway, playing a crucial role in regulating various biological processes, including cellular differentiation and proliferation. Due to its selective action, ALK5-IN-33 is a valuable tool in research applications focused on fibrosis, cancer, and developmental biology. -
ALK5 Inhibitor
ALK5-IN-80 is a selective inhibitor of ALK5, exhibiting an IC50 value of 3.7 nM. This compound effectively antagonizes ALK5 signaling pathways, making it a valuable tool for cancer research. Its ability to selectively inhibit ALK5 activity allows for investigations into the role of this pathway in oncogenesis and tumor progression. -
TGF-β Agonist
KRFK is a TGF-β agonist peptide derived from thrombospondin-1 (TSP-1) that activates the TGF-β pathway. This compound enhances TGF-β-mediated signaling and its downstream effects, operating independently of TSP receptors, including CD47 and CD36. KRFK is ideally suited for research applications involving chronic ocular surface inflammatory disorders. -
Fusion Protein
Rinvatercept is a fusion protein targeting the extracellular domains of human ACVR2A and ACVR2B, linked to an immunoglobulin G1 (IgG1) Fc fragment via a G3 peptide linker. This compound is designed for research applications focused on neuromuscular diseases by modulating signaling pathways associated with muscle and nerve function. Its unique structure enhances stability and therapeutic potential, making it a valuable tool for studying related biological mechanisms. -
TGF-β Receptor Activator
Phenamil is a TGF-β receptor activator that plays a crucial role in bone repair by promoting the activity of the bone morphogenetic protein signaling pathway. This compound not only enhances osteogenic differentiation but also has the potential to induce adipogenesis. Employing a specialized 3D scaffold strategy can further enhance its ability to induce osteogenic differentiation while mitigating adipogenic effects, making it valuable for research in regenerative medicine and stem cell biology. -
ALK-5 Inhibitor
ALK5-IN-31 is a selective inhibitor of ALK-5, with an IC50 value of ≤10 nM, that effectively disrupts TGF-β-induced SMAD signaling pathways. This compound demonstrates potential anti-tumor activity in vivo and may be instrumental in the research of proliferative diseases, including cancer, fibrotic disorders, and systemic sclerosis. Its targeted inhibition of ALK-5 makes it a valuable tool for investigating the therapeutic mechanisms in fibrosis and tumorigenesis. -
TGFβRI Inhibitor
TGFβRI-IN-5 is a selective inhibitor of TGFβRI, exhibiting a potent inhibitory activity with an IC50 of 0.08 μM. This compound demonstrates significant anticancer efficacy, showing 5–7 times greater activity compared to reference agents across a range of tested cell lines. Furthermore, TGFβRI-IN-5 promotes apoptosis and effectively arrests the cell cycle at the G2/M phase, making it a valuable tool for investigating TGFβ signaling in cancer research and therapeutic applications. -
Anti-fibrotic agent
TGFβ1-IN-2 is a diarylacylhydrazones derivative primarily acting as an anti-fibrotic agent through the inhibition of TGF-β1 signaling. It effectively suppresses fibroblast activation and proliferation, making it a valuable tool for studying idiopathic pulmonary fibrosis (IPF) and related fibrotic disorders. This compound has potential applications in investigating therapeutic strategies for managing fibrosis. -
Anti-fibrotic agent
TGFβ1-IN-3 is a diarylacylhydrazones derivative that acts as an anti-fibrotic agent by effectively inhibiting the activation and proliferation of fibroblasts. This compound is particularly valuable for research on idiopathic pulmonary fibrosis (IPF), where it can help elucidate the mechanisms and treatment options for fibrotic diseases. Its role in modulating fibroblast activity makes TGFβ1-IN-3 a useful tool in understanding fibrogenesis and developing therapeutic strategies. -
ALK5 Inhibitor
ALK5-IN-7 is a selective inhibitor of ALK5, a key receptor in the TGF-β signaling pathway. This compound modulates cell proliferation, differentiation, and apoptosis, making it valuable for investigating various TGF-β-related diseases. Research applications include studies on tumors, fibrotic diseases, inflammatory disorders, and autoimmune conditions. -
Activin Antagonist
NUCC-555 is an activin antagonist that targets the Activin A binding pocket, specifically interacting with critical residues such as Trp25, Trp28, Phe55, Tyr93, Lys103, and Asn107. This compound effectively inhibits Activin A-mediated activation of hepatic stellate cells (HSCs), promoting liver regeneration and slowing the progression of fibrosis in chronic liver disease models. Additionally, NUCC-555 suppresses ovarian cell proliferation driven by Activin A and reduces follicle-stimulating hormone (FSH) levels in ovariectomized mouse models, making it a valuable tool for research in liver and reproductive health. -
BMPR2 Inhibitor
CDD-1431 is a selective inhibitor of Bone Morphogenetic Protein Receptor 2 (BMPR2), exhibiting a Kiapp value of 20.6 nM. This compound effectively suppresses BMP-responsive element (BRE)-reporter activity, with an IC50 of 4.87 μM, demonstrating its potency in modulating BMP signaling pathways. BMPR2 plays a crucial role in various cellular processes across multiple tissues, including the kidney, skeletal muscle, heart, and reproductive organs, and its inhibition can provide insights into mechanisms underlying ectopic bone formation and related pathologies. -
ALK5 Inhibitor
ALK5-IN-85 is an inhibitor of TGFβRI (ALK5) with an IC50 of less than 100 nM. This compound exhibits significant potential in the study of respiratory diseases such as idiopathic pulmonary fibrosis, asthma, chronic obstructive pulmonary disease (COPD), and lung cancer. Additionally, ALK5-IN-85 may be applicable in researching dermal and ocular fibrotic conditions, making it a valuable tool for understanding and targeting fibrotic pathways in various therapeutic areas. -
Inactive Control
KQFK is an inactive control of the active peptide KRFK, which is derived from thrombospondin-1 (TSP-1) and is known to activate transforming growth factor-beta (TGF-β). This control serves as a valuable tool for validating experimental results involving KRFK in studies of TGF-β signaling pathways. It can be employed in various biological assays to ascertain the specificity and effects of KRFK in cellular and molecular research. -
ALK-5/2 Inhibitor
ALK5-IN-25 is a potent inhibitor of ALK-5 and ALK-2, exhibiting an IC50 of ≤10 nM. This compound interferes with TGF-β signaling pathways, making it a valuable tool for cancer research. ALK5-IN-25 is essential for studying the role of ALK-5 and ALK-2 in tumor progression and evaluating potential therapeutic strategies targeting these pathways. -
ALK2 Inhibitor
M4K2308 is a selective inhibitor of ALK2, featuring an IC50 of 2 nM. This compound demonstrates remarkable selectivity for ALK2 compared to ALK5, with an IC50 of 224 nM. M4K2308 is valuable for research applications focused on diffuse intrinsic pontine glioma (DIPG), allowing for deeper understanding of this challenging neuro-oncological condition. -
TGFβR1 Inhibitor Prodrug
TGFβ-IN-3 is a prodrug that selectively inhibits TGFβR1. It exhibits enhanced selective drug release within tumors, resulting in a significant 2.2-fold increase in the tumor-to-blood concentration ratio. This compound is valuable for researching colon cancer and its associated signaling pathways, providing insights into potential therapeutic strategies targeting the TGFβ axis in tumor microenvironments. -
ALK-5/2 Inhibitor
ALK5-IN-27 is a potent inhibitor of ALK-5, exhibiting an IC50 of ≤10 nM. Additionally, this compound demonstrates selectivity for ALK-2, with a selectivity ratio of ALK-2 to ALK-5 of ≤10. ALK5-IN-27 is valuable for studying TGF-β signaling pathways and investigating its role in various fibrotic and oncogenic processes. -
BMP Upregulator
BUR1 is a bone morphogenetic protein (BMP) upregulator that primarily activates BMPRII signaling with an EC50 of 98 nM. It effectively induces the expression of BMP2 and PTGS2, making it a valuable tool in studies related to BMP signaling pathways. Additionally, BUR1 has been shown to reverse pulmonary arterial pressure in monocrotaline-induced rat models, highlighting its potential applications in cardiovascular and pulmonary research. -
TGF-β1 inhibitor
Pixofisiran is a small interfering RNA (siRNA) that specifically inhibits transforming growth factor-beta 1 (TGF-β1). This compound plays a significant role in modulating fibrosis and inflammation, making it a valuable tool for research into these biological processes. Applications include studies related to cancer, tissue repair, and the mechanistic exploration of TGF-β1 signaling pathways. -
TGF-β Receptor
Maohuoside A targets the TGF-β receptor and is derived from E. koreanum. This compound has shown potent activity in promoting osteogenesis, particularly through its effects on bone marrow-derived mesenchymal stem cells. Maohuoside A enhances osteogenic differentiation by modulating bone morphogenetic protein (BMP) and MAPK signaling pathways, making it valuable for research in bone formation and regenerative medicine. -
ALK5 Inhibitor
J-1063 is a potent and selective inhibitor of ALK5, demonstrating an IC50 of 0.039 µM. This compound exerts anti-fibrotic effects through the inhibition of inflammatory infiltration, collagen deposition, and hepatocyte necrosis. J-1063 is valuable for research focused on liver fibrosis and associated cellular mechanisms. -
Anti-Liver Fibrosis Agent
MCA17-1 is an anti-liver fibrosis agent that demonstrates enhanced bioactivity compared to the positive control obeticholic acid (OCA). This compound serves as a valuable tool in research aimed at understanding liver fibrosis mechanisms and developing therapeutic strategies. Its superior efficacy positions MCA17-1 as a key candidate for studies focused on liver health and potential fibrosis reduction. -
ALK2 Inhibitor
M4K2306 is a selective inhibitor of activin receptor-like kinase-2 (ALK2), exhibiting an IC50 of 7 nM. This compound demonstrates significant blood-brain permeability with a brain-to-plasma ratio of 75.6, making it a valuable tool for studying the role of ALK2 in neurological conditions. Its selective inhibition of ALK2 positions M4K2306 for research applications in understanding signaling pathways related to developmental processes and various diseases.
