Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Smad Inhibitor
(14S,15R)-14-Deoxyoxacyclododecindione is a selective inhibitor of the TGF-β-dependent Smad2/3 and IL-4-dependent STAT6 signaling pathways, exhibiting IC50 values of 90 nM and 20 nM, respectively. This compound has significant potential for applications in cancer research and the study of fibrotic diseases by modulating key signaling events. Its ability to inhibit these pathways makes it a valuable tool for investigating the role of TGF-β and IL-4 in various biological processes. -
TGF-β Inhibitor
TGF-βRI inhibitor 3 is a selective inhibitor of the TGF-β receptor type I (ALK5), designed to effectively disrupt TGF-β signaling pathways. It demonstrates notable inhibitory activity with IC50 values of 0.63 μM against ALK5 and 13 μM against c-Src kinase. This compound is valuable for research applications targeting fibrosis, cancer progression, and other TGF-β-mediated biological processes. -
TGF-beta/Smad Inhibitor
RepSox hydrochloride is a highly selective inhibitor of transforming growth factor-β receptor I (TGF-β-RI) and activin-like kinase 5 (ALK5). It effectively inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. This reagent is valuable for investigating the roles of TGF-β signaling in obesity and metabolic disorders, including type 2 diabetes. -
PDE4 inhibitor
Hesperetin, a selective phosphodiesterase (PDE)4 inhibitor, is present in the traditional Chinese medicine, ?€?Chen Pi.?€? Hesperetin is a citrus flavonoid that has been reported to lower plasma cholesterol. Hesperetin reduces the transcription of ACAT-2 mRNA in Hep-G2 cells and reduces ApoB protein synthesis in a dose-dependent manner. It also is a potential therapy for carcinoid cancer. -
BMP type I receptor inhibitor
LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50??500 nM). -
BMP signaling inhibitor
LDN193189 HCl (DM-3189) is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cell lines, respectively, 200-fold selectivity for BMP versus TGF-β. -
BMP4 signaling agonist
BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC50 value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. -
Smad3/HIF-α Dual Target PROTAC
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine functions as a dual-target PROTAC, effectively inducing ubiquitination and degradation of Smad3 while simultaneously enhancing HIF-α protein levels. This compound exhibits multi-pathway anti-fibrotic activity and renal protective properties, making it valuable for research on renal anemia. Additionally, it has potential applications in studying prostate cancer and other malignancies, contributing to a deeper understanding of cancer biology and treatment modalities. -
PPAR agonist
Lobeglitazone sulfate is a novel thiazolidinedione and an orally active agonist of peroxisome proliferator-activated receptors (PPARs), with EC50 values of 137.4 nM for PPARγ and 546.3 nM for PPARα. It also acts as an inhibitor of the ERK/JNK/Smad/NF-κB signaling pathways. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic activities, supporting its potential in the treatment of metabolic and inflammatory diseases. -
PPAR agonist
Lobeglitazone is a novel thiazolidinedione-class compound and an orally active dual agonist of peroxisome proliferator-activated receptors (PPARs), with EC₅₀ values of 137.4 nM for PPARγ and 546.3 nM for PPARα. In addition to its metabolic effects, Lobeglitazone functions as an inhibitor of multiple pro-inflammatory and pro-fibrotic signaling pathways, including ERK, JNK, Smad, and NF-κB. Lobeglitazone exhibits a broad range of pharmacological activities, including anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic effects. These properties make it a promising candidate for therapeutic research in metabolic syndrome, type 2 diabetes, cardiovascular disease, and fibrosis-related conditions. -
CBSI inhibitor
MY-673 is a colchicine binding site inhibitor (CBSI) that disrupts microtubule dynamics by inhibiting tubulin polymerization. In addition to its antimitotic effects, MY-673 suppresses the ERK signaling pathway, which leads to modulation of SMAD4 protein expression within the TGF-β/SMAD signaling axis. These combined actions result in potent inhibition of cancer cell proliferation and migration, and the induction of apoptosis, both in vitro and in vivo. MY-673 holds promise as a therapeutic candidate for targeting cancers driven by aberrant microtubule dynamics and dysregulated TGF-β/ERK signaling. -
BMP receptor agonist
SY-LB-35 is a potent agonist of bone morphogenetic protein (BMP) receptors, capable of activating both canonical and non-canonical signaling pathways. In the C2C12 myoblast cell line, SY-LB-35 significantly enhances cell proliferation and viability, promoting cell cycle progression by increasing the proportion of cells in the S and G2/M phases. Mechanistically, it activates the canonical Smad pathway as well as non-canonical PI3K/Akt, ERK, p38, and JNK signaling cascades. These properties make SY-LB-35 a valuable tool for studying BMP-related cellular processes and a potential therapeutic candidate for tissue regeneration and muscle repair. -
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.
