TGF-β/Smad Inhibitors

Cat. No.

A47971

CAS No.

733806-89-8

TGFBR1-IN-2

TGFBR1-IN-2 is a potent TGFBR1 inhibitor that targets the transforming growth factor-beta signaling pathway. This compound exhibits significant antibacterial activity, particularly against Mycobacterium tuberculosis. TGFBR1-IN-2 demonstrates effective inhibition of both non-replicating and persistent forms of the bacteria, making it a valuable tool for research on tuberculosis treatment and the modulation of immune responses. Additionally, it serves as a substrate for cytochrome P450 enzymes, which may influence its metabolic profile in biological systems.

Cat. No.

A57587

CAS No.

69640-38-6

Pentachloropseudilin

Synonyms: Antibiotic A 15104 Y; PClP

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.

Cat. No.

A64212

CAS No.

2419918-89-9

Dalutrafusp alfa

Synonyms: AGEN-1423; GS-1423

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.

Cat. No.

A84792

CAS No.

2828431-89-4

A 83-01 sodium

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.

Cat. No.

A84843

CAS No.

1001080-50-7

Sotatercept

Synonyms: ACE-011; MK-7962

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.

Cat. No.

A84844

CAS No.

1801333-55-0

PF-06952229

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.

Cat. No.

A84845

CAS No.

2348795-14-0

TGFβ1-IN-1

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.

Cat. No.

A84846

CAS No.

3034216-44-6

CDD-1653

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.

Cat. No.

A84847

CAS No.

1352610-25-3

Vactosertib Hydrochloride

Synonyms: EW-7197 Hydrochloride; TEW-7197 Hydrochloride

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.

Cat. No.

A84848

CAS No.

1918149-01-5

Bintrafusp alfa

Synonyms: M7824; MSB0011359C

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.

Cat. No.

A84849

CAS No.

2442519-59-5

THRX-144644

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.

Cat. No.

A84850

CAS No.

10245-81-5

Pentabromopseudilin

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.

Cat. No.

A84851

CAS No.

2253719-35-4

SY-LB-57

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.

Cat. No.

A84852

CAS No.

868612-83-3

IN-1130

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.

Cat. No.

A84853

CAS No.

1807631-83-9

CJJ300

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.

Cat. No.

A84854

CAS No.

2705900-81-6

ALK5-IN-8

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.

Cat. No.

A84855

CAS No.

2647949-48-0

Ontunisertib

Synonyms: AGMB-129

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.

Cat. No.

A84856

CAS No.

1251838-01-3

Vicatertide

Synonyms: SB-01

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.

Cat. No.

A84857

CAS No.

2173389-57-4

Zilurgisertib

Synonyms: INCB-000928; NBU-928

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.

Cat. No.

A84858

CAS No.

1117684-36-2

AZ12799734

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.

Cat. No.

A84859

CAS No.

2748337-86-0

AZ12601011

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.

Cat. No.

A84860

CAS No.

259870-32-1

TGFβ-IN-5

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.

Cat. No.

A84861

CAS No.

2001559-19-7

BMS-986260

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.

Cat. No.

A84862

CAS No.

1976038-41-1

TP-008

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.

Cat. No.

A84863

CAS No.

2763602-67-9

TGFβRI-IN-3

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.