TGF-β/Smad Inhibitors

Cat. No.

A34561

CAS No.

3034215-86-3

CDD-1115

CDD-1115 is a selective inhibitor of Bone Morphogenetic Protein Receptor Type 2 (BMPR2) with an IC50 of 1.8 nM and an apparent Ki of 6.2 nM. This compound inhibits BMP-mediated gene expression, which plays a critical role in various cellular processes across diverse tissues, including the kidney, skeletal muscle, heart, and reproductive organs. CDD-1115 is ideal for investigating the regulatory effects of BMP signaling and its involvement in ectopic bone formation.

Cat. No.

A35980

CAS No.

1899061-36-9

(14S,15R)-14-Deoxyoxacyclododecindione

(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.

Cat. No.

A36978

CAS No.

1629138-41-5

SRI-011381

SRI-011381 is an orally active agonist of the TGF-β/Smad signaling pathway. It has been shown to exhibit neuroprotective effects, making it a valuable tool for research in neurobiology and regenerative medicine. This compound can be utilized to investigate the role of TGF-β in various cellular processes and potential therapeutic applications in neurodegenerative diseases.

Cat. No.

A36979

CAS No.

1373715-00-4

Luspatercept

Synonyms: ACE-536; luspatercept–aamt

Luspatercept is a recombinant modified ActRIIB fusion protein that functions as a Smad2/3 inhibitor. It selectively binds to transforming growth factor β (TGF-β) superfamily ligands, including GDF11, thereby inhibiting Smad2/3 signaling. This compound promotes the maturation of erythroid precursors and increases erythrocyte numbers, making it a valuable tool for research into anemia and related erythropoietic disorders.

Cat. No.

A36986

CAS No.

1443994-98-6

Mongersen sodium

Synonyms: GED-0301 sodium

Mongersen sodium is a targeted SMAD7 antisense oligonucleotide that functions to restore TGF-β1 activity, resulting in the inhibition of inflammatory signaling pathways. This compound has demonstrated efficacy in attenuating experimental colitis resembling Crohn's disease in mouse models. It is a valuable tool for studying inflammatory bowel disease mechanisms and the modulation of TGF-β signaling in various research applications.

Cat. No.

A36989

CAS No.

521985-36-4

SIS3 free base

SIS3 free base is a potent and selective inhibitor of Smad3 phosphorylation. It significantly inhibits the myofibroblast differentiation of fibroblasts induced by TGF-β1 while leaving the phosphorylation of Smad2 unaffected. This specificity makes SIS3 free base a valuable tool for studying the role of Smad3 in cellular processes associated with fibrosis and other TGF-β1 mediated pathways.

Cat. No.

A36992

CAS No.

577-38-8

Flavanomarein

Flavanomarein is a potent inhibitor of Syk and NF-κB p65, as well as a modulator of TGF-β1/Smad signaling pathways. This compound exhibits cytoprotective, anti-inflammatory, and antioxidant activities, enhancing AKT phosphorylation while regulating key proteins such as PKC-δ, P85α, PKC-β1, Sirt1, Bcl-2, and ICAD. Flavanomarein also inhibits the nuclear translocation of NF-κB p65 and modulates epithelial-mesenchymal transition (EMT) markers, promoting proliferation in HK-2 cells and protecting neuronal cells from 6-OHDA-induced neurotoxicity. This compound is valuable for research on Parkinson's disease and diabetic nephropathy.

Cat. No.

A36996

CAS No.

925681-61-4

Trabedersen

Synonyms: AP 12009

Trabedersen is an antisense oligodeoxynucleotide that specifically targets and inhibits TGF-β2, a key regulator in the TGF-beta/Smad signaling pathway. This reagent is critical for research in malignant brain tumors and various solid tumors, including those affecting the skin, pancreas, and colon, which exhibit overexpression of TGF-β2. By modulating this pathway, Trabedersen offers insights into tumor biology and potential therapeutic strategies.

Cat. No.

A36998

CAS No.

2387678-02-4

TGFβ-IN-2

TGFβ-IN-2 is an orally active inhibitor of TGF-β, targeting its signaling pathways. This compound effectively suppresses TGF-β-induced expression of key proteins such as COL1A1, α-SMA, and p-Smad3 in vitro. TGFβ-IN-2 exhibits significant anti-fibrotic effects in a Bleomycin-induced pulmonary fibrosis model, making it a valuable tool for investigating the mechanisms and potential treatments of pulmonary fibrosis.

Cat. No.

A37001

CAS No.

1443994-46-4

Mongersen

Synonyms: GED-0301

Mongersen is a targeted SMAD7 antisense oligonucleotide that restores TGF-β1 activity, thereby inhibiting inflammatory pathways. This compound has demonstrated the ability to attenuate experimental colitis resembling Crohn's disease in murine models. Its application is particularly relevant in studying inflammation and fibrosis related to gastrointestinal disorders.

Cat. No.

A37003

CAS No.

162401-62-9

DGM

DGM is a specific inhibitor of the TGF-β1/Smad signaling pathway, exhibiting notable antifibrotic properties. It effectively inhibits the epithelial-mesenchymal transition (EMT) in alveolar epithelial cells, thereby slowing the progression of pulmonary fibrosis in vivo. DGM reduces lung inflammation, enhances lung function, and minimizes extracellular matrix remodeling, making it a valuable tool for research on idiopathic pulmonary fibrosis (IPF) and other EMT-related diseases.

Cat. No.

A37010

CAS No.

2785430-90-0

ALK5-IN-34

ALK5-IN-34 is a selective inhibitor of activin receptor-like kinase 5 (ALK5), exhibiting potent activity with an IC50 value of ≤10 nM. This compound effectively reduces tumor proliferation, making it a valuable tool for research on proliferative diseases, including various cancer types. ALK5-IN-34 may facilitate investigations into the mechanisms underlying cancer progression and therapeutic interventions targeting the ALK5 pathway.

Cat. No.

A37011

CAS No.

846546-36-9

P17 Peptide

P17 Peptide is a selective inhibitor of human TGF-β1, functioning by blocking its activity. This peptide is valuable for studying the role of TGF-β1 in various biological processes and disease states, including fibrosis and cancer. Its inhibitory effects facilitate research into therapeutic strategies targeting TGF-β signaling pathways.

Cat. No.

A37016

CAS No.

2414315-95-8

DT-6

DT-6 is a selective inhibitor of TGF-β1, a key regulator of cellular processes related to fibrosis and cancer progression. By inhibiting TGF-β1, DT-6 effectively disrupts M2 macrophage-induced epithelial to mesenchymal transition (EMT) and inhibits the invasive migration of cancer cells. This compound is valuable for research applications focused on cancer biology and related therapeutic interventions.

Cat. No.

A37018

CAS No.

2179222-27-4

ISTH0036

ISTH0036 is a selective antisense oligonucleotide targeting transforming growth factor beta 2 (TGF-β2). It exhibits inhibitory activity against TGF-β2 expression, making it a valuable tool for investigating the pathophysiological mechanisms of primary open-angle glaucoma (POAG) and wet age-related macular degeneration. This reagent is suitable for both in vitro and in vivo studies aimed at understanding the role of TGF-β2 in these ocular conditions.

Cat. No.

A37020

CAS No.

959610-24-3

Myristoyl tetrapeptide-12

Myristoyl tetrapeptide-12 is a specific activator of SMAD2, promoting the recruitment of SMAD3 to DNA. This peptide exhibits significant biological activity in stimulating hair growth, with notable effects on eyelash enhancement. Its applications are particularly relevant in research focusing on hair follicle biology and regenerative medicine.

Cat. No.

A37022

CAS No.

3100351-69-4

TGF-β/Smad-IN-3

TGF-β/Smad-IN-3 is a potent inhibitor of the TGF-β/Smad signaling pathway and MAPK pathway. This compound demonstrates significant anti-pulmonary fibrosis activity by inhibiting collagen deposition resulting from TGF-β1, with an IC50 of 3.21 μM. Additionally, TGF-β/Smad-IN-3 effectively reduces the expression of α-SMA, COL1A1, and FN in TGF-β1-induced CCC-HPF-1 cells, while also significantly reducing cell migration. This reagent is valuable for research focused on pulmonary fibrosis and related fibrosis-related mechanisms.

Cat. No.

A37029

CAS No.

3097194-50-5

TGF-β1/Smad-IN-1

TGF-β1/Smad-IN-1 is a potent inhibitor of the TGF-β1/Smad signaling pathway, which plays a crucial role in the regulation of fibrotic processes. This compound effectively reduces the expression of fibrosis markers, such as α-SMA and COL1A1, induced by TGF-β1, demonstrating significant antifibrotic activity. TGF-β1/Smad-IN-1 is valuable for research applications focused on hepatic fibrosis and related fibrotic disorders.

Cat. No.

A37030

CAS No.

162559-45-7

H-Leu-Ser-Lys-Leu-OH

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.

Cat. No.

A37033

CAS No.

1253691-50-7

PXS 64

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.

Cat. No.

A37036

CAS No.

2785430-84-2

ALK5-IN-28

ALK5-IN-28 is a selective inhibitor of ALK-5 with an IC50 of ≤ 10 nM, effectively blocking TGF-β-induced SMAD signaling pathways. This compound demonstrates significant potential in inhibiting tumor growth in vivo, making it valuable for research into proliferative diseases such as cancer. Its precise action on the ALK-5 target allows for targeted investigations into therapeutic strategies against TGF-β-mediated tumorigenesis.

Cat. No.

A37039

CAS No.

2785430-88-6

ALK5-IN-32

ALK5-IN-32 is a selective inhibitor of ALK-5, exhibiting an IC50 range of 10 nM to 100 nM. This compound effectively inhibits TGF-β-induced SMAD signaling pathways, thereby demonstrating potential in the inhibition of tumor growth in vivo. ALK5-IN-32 is valuable for research into proliferative diseases, including cancer, fibrotic disorders, and systemic sclerosis.

Cat. No.

A40754

CAS No.

1352609-28-9

EW-7195

EW-7195 is a selective inhibitor of ALK5 (TGFβR1), exhibiting an IC50 of 4.83 nM and demonstrating over 300-fold selectivity for ALK5 compared to p38α. This compound effectively inhibits TGF-β1-induced Smad signaling pathways, epithelial-to-mesenchymal transition (EMT), and the metastatic spread of breast tumors to the lung. EW-7195 is valuable for research applications focused on TGF-β signaling, cancer metastasis, and understanding the molecular mechanisms of fibrosis and EMT.

Cat. No.

A40827

CAS No.

2883580-95-6

J-1149

J-1149 is a potent inhibitor of ALK5 (activin receptor-like kinase 5), exhibiting an IC50 value of 0.017 μM. Additionally, J-1149 demonstrates weak inhibitory activity against p38α MAP kinase, with an IC50 of 0.435 μM. This compound is relevant for research into liver fibrosis and related fibrotic diseases, providing a valuable tool for investigating therapeutic strategies targeting TGF-β signaling pathways.

Cat. No.

A42470

CAS No.

1825371-51-4

Smurf1 modulator-1

Smurf1 modulator-1 is a selective inhibitor of Smad ubiquitination regulatory factor 1 (Smurf1), with an IC50 of 180 nM. This compound acts by blocking the ubiquitin ligase activity of Smurf1, thereby modulating Smad protein degradation. Its primary applications include studies of cellular signaling pathways and investigations into the role of Smurf1 in cancer and fibrosis.