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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
ALK2 Inhibitor
ALK2-IN-6 is a selective inhibitor of ALK2, exhibiting an IC50 value of 9 nM. This compound is instrumental in investigating the biological role of ALK2 in various contexts, particularly in the study of diffuse intrinsic pontine glioma. Researchers may utilize ALK2-IN-6 to explore its therapeutic potential and molecular mechanisms associated with ALK2 signaling pathways. -
TGF-β1 Inhibitor
TJN-331 is a potent, orally active inhibitor of TGF-β1, targeting the TGF-β signaling pathway. This compound demonstrates significant therapeutic potential by ameliorating anti-glomerular basement membrane nephritis in rat models, reducing extracapillary proliferation in glomeruli. Additionally, TJN-331 inhibits mesangial expansion in experimental IgA nephropathy in ddY mice, making it a valuable tool for researching nephritis and IgA nephropathy. -
ALK5 Inhibitor
ALK5-IN-6 is a selective inhibitor of ALK5, a key component in the TGF-β signaling pathway. This compound effectively modulates the biological activities of TGF-β, which is crucial for regulating cell proliferation, differentiation, and apoptosis. ALK5-IN-6 is valuable for research into TGF-β-related conditions, including various tumors, fibrotic diseases, inflammatory responses, and autoimmune disorders. -
TGF-βR1 Inhibitor
TGFβRI-IN-4 is a potent and orally bioavailable inhibitor of the TGF-β receptor type I (TGFβRI), demonstrating IC50 values of 44 nM and 42.5 nM against ALK5 and NIH3T3 cell lines, respectively. This compound effectively inhibits TGF-β signaling, leading to suppression of tumor growth and reduction in tumor weight in xenograft models. TGFβRI-IN-4 is particularly valuable for research into cancer biology and therapeutic interventions targeting the TGF-β pathway. -
BMPR2 Kinase Inhibitor
CDD-1281 is a potent and selective inhibitor of the BMPR2 kinase, demonstrating an IC50 value of 1.2 nM. This compound effectively inhibits BMP-mediated gene expression, making it valuable for research applications focused on BMP signaling pathways and their implications in various biological processes. -
ALK5 Inhibitor
ALK5-IN-82 is a potent and selective inhibitor of activin receptor-like kinase 5 (ALK5), demonstrating an IC50 value of 9.1 nM. This compound effectively reduces the expression of α-smooth muscle actin, collagen I, and tissue inhibitor of metalloproteinase 1 in transforming growth factor-β-induced human umbilical vein endothelial cells. ALK5-IN-82 is particularly relevant for the study of cardiac fibrosis and its associated pathways, making it a valuable tool in cardiovascular research applications. -
Type I TGF-β Receptor Kinase Inhibitor
LY550410 is a small-molecule ATP-competitive inhibitor targeting the type I TGF-β receptor kinase. By inhibiting this receptor, LY550410 modulates TGF-β signaling pathways, influencing gene expression and regulating cell growth. This compound is of particular interest for research applications related to cancer biology and therapeutic interventions. -
TGF-β Receptor Inhibitor
Nicousamide is a potent TGF-β receptor II inhibitor that effectively prevents phosphorylation of this receptor. This compound is instrumental in investigating renal fibrosis and its underlying mechanisms, particularly in animal models of diabetic nephropathy. Researchers can utilize Nicousamide to explore therapeutic strategies aimed at mitigating fibrotic processes in kidney disease.
