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TGF-β/Smad inhibitors block transforming growth factor beta (TGF-β) signaling at its receptor kinases or Smad proteins. TGF-β binds a type II receptor kinase, which then phosphorylates the type I receptor, activin receptor-like kinase 5 (ALK5). The activated type I receptor phosphorylates Smad2 and Smad3, which join Smad4 and move into the nucleus to regulate transcription. SB 431542 and A 83-01 inhibit ALK5 together with the related receptors ALK4 and ALK7. RepSox and galunisertib also target the TGF-β type I receptor, while SIS3 blocks Smad3 downstream. LDN193189 instead inhibits ALK2 and ALK3, type I receptors for bone morphogenetic proteins.
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.
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.
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 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.
Synonyms: ALK2-IN-4
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.
Synonyms: ALK2-IN-4 succinate
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.
Synonyms: ACE-031
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.
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.
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.
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.
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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.
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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-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-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-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-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.
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.
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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-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.
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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.
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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.
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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.
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-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.
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.
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