TGF-β/Smad Inhibitors: SB 431542 & RepSox

Cat. No.: A84893

CAS No.: 2883813-58-7

TGFβ1-IN-3

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.

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$65.00

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$165.00

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Cat. No.: A84894

CAS No.: 2657720-07-3

ALK5-IN-7

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.

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Cat. No.: A84895

CAS No.: 1060469-90-0

NUCC-555

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.

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Cat. No.: A84896

CAS No.: 3034216-31-1

CDD-1431

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.

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Cat. No.: A84897

CAS No.: 2766583-86-0

ALK5-IN-85

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.

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Cat. No.: A84898

CAS No.: 162290-88-2

KQFK

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.

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Cat. No.: A84899

CAS No.: 2785430-81-9

ALK5-IN-25

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.

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Cat. No.: A84900

CAS No.: 3034840-18-8

M4K2308

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.

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Cat. No.: A84901

CAS No.: 2857845-34-0

TGFβ-IN-3

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.

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Cat. No.: A84902

CAS No.: 2785430-83-1

ALK5-IN-27

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.

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Cat. No.: A84903

CAS No.: 23000-46-6

BUR1

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.

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$105.00

5 mg

$270.00

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Cat. No.: A84904

CAS No.: 1152798-48-5

Pixofisiran

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.

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Cat. No.: A84905

CAS No.: 128988-55-6

Maohuoside A

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.

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$40.00

5 mg

$100.00

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Cat. No.: A84906

CAS No.: 2374772-46-8

J-1063

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.

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Cat. No.: A84907

CAS No.: 2661480-70-0

MCA17-1

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.

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Cat. No.: A84908

CAS No.: 3034840-25-7

M4K2306

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.

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Cat. No.: A84909

CAS No.: 2600795-23-9

ALK2-IN-6

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.

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$155.00

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$395.00

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Cat. No.: A84910

CAS No.: 883560-84-7

TGFβ-IN-1

TGFβ-IN-1 is a selective inhibitor of the transforming growth factor-β (TGF-β) receptor, targeting the TGF-β signaling pathway. This compound exhibits potent antitumor activity by suppressing tumor growth and metastasis. TGFβ-IN-1 is utilized in cancer research to investigate the molecular mechanisms underlying tumor progression and to explore potential therapeutic strategies for TGF-β-related malignancies.

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Cat. No.: A84911

CAS No.: 219964-53-1

TJN-331

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.

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Cat. No.: A84912

CAS No.: 2657720-04-0

ALK5-IN-6

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.

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Cat. No.: A84913

CAS No.: 2421135-03-5

TGFβRI-IN-4

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.

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Cat. No.: A84914

CAS No.: 402824-96-8

HCTZ-CH2-HCTZ

HCTZ-CH2-HCTZ is an isomer of hydrochlorothiazide (HCTZ), a thiazide-class diuretic that functions primarily by inhibiting the transforming growth factor-beta (TGF-β)/Smad signaling pathway. This compound exhibits biological activity pertinent to fluid regulation and vascular integrity, making it valuable in research applications focused on cardiovascular biology and renal function. Its unique structure may provide insights into the mechanism of action and therapeutic potential of diuretics in various pathological conditions.

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Cat. No.: A84915

CAS No.: 3034215-91-0

CDD-1281

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.

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Cat. No.: A84916

CAS No.: 3001361-04-9

ALK5-IN-82

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.

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Cat. No.: A84918

CAS No.: 737791-20-7

LY550410

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.

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