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Product Name
Application
Product Information
Citations
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ALK4/ALK5 inhibitor
EW-7197 is a highly potent, selective, and orally bioavailable TGF-β I receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively- Bordignon P, .et al. , Cell Rep, 2019, Aug 27;28(9):2358-2372 PMID: 31461652
- Morita T, .et al. , Mol Cancer Res, 2018, May;16(5):880-893 PMID: 29330296
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ALK5 inhibitor
RepSox (SJN 2511) is a selective inhibitor of the TGF-β type I receptor ALK5 (IC50 values are 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding respectively).- Katarzyna Blaszczyk, .et al. , Exp Mol Med, 2025, Feb;57(1):131-150 PMID: 39741186
- Wojciech J Szlachcic, .et al. , iScience, 2022, Jul 15;25(7) PMID: 35756892
- Xu H, .et al. , Cancer Lett, 2020, Mar 1;472:151-164 PMID: 31846689
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ALK inhibitor
LDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation.- Lei Wang, .et al. , Theriogenology, 2023, Feb;197:167-176 PMID: 36525856
- Trang Thi Huyen Dang, .et al. , Mol Cell Biochem, 2021, May;476(5):2085-2097 PMID: 33517521
- Shizu Aikawa, .et al. , EMBO J, 2017, Jul 14; 36(14): 2146-2160 PMID: 28588064
- HIROTAKA SOMEYA, .et al. , Int J Mol Med, 2015, May; 35(5): 1169-1178 PMID: 25739055
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TGF-beta/Smad inhibitor
GW788388 is a potent, orally active and selective inhibitor of transforming growth factor beta receptor I (TGF-βR1) (activin receptor-like kinase 5, ALK5).- Lisa J. Randall, .et al. , Sci Rep, 2025, 15: 27260 PMID: 40715237
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TGF-β inhibitor
ITD-1 is a novel and highly selective TGFβ pathway inhibitor. ITD-1 molecule turns stem cells into heart cells.- M. C. Wilkes, .et al. , Nat Commun, 2020, 11: 3344 PMID: 32620751
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TGF-beta/Smad inhibitor
SB 431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I ALK receptors ALK4, ALK5, and ALK7 .- Mehri Moradi, .et al. , Nat Commun, 2025, 16: 8724 PMID: 41028013
- Neha Jadhav Giridhar, .et al. , Biol Open, 2025, Sep 15;14(9):bio062196 PMID: 40814270
- Sebastian Held, .et al. , Cell Rep, 2025, Jan 28;44(1):115107 PMID: 39709600
- Yuri Nagaoka, .et al. , Arch Biochem Biophys, 2024, Jan:751:109824 PMID: 37984759
- Huong Pham, .et al. , Biotechnol Bioprocess Eng, 2020, ID: 222137835
- Tamara Chamberlin, .et al. , FASEB J, 2020, Jun;34(6):8611-8624 PMID: 32359100
- Satoshi Endo, .et al. , Nutr Res, 2019, 4 November PMID: 31767206
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Smad3 inhibitor
SIS3 is a novel specific inhibitor of Smad3. It has effect on transforming growth factor-beta1-induced extracellular matrix expression.- Miao Deng, .et al. , ACS Appl Mater Interfaces, 2021, Apr 21;13(15):18033-18046 PMID: 33834754
- Wei P, .et al. , Cell Death Dis, 2019, Sep 11;10(9):670 PMID: 31511493
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BMP inhibitor
DMH-1 is a selective inhibitor of the bone morphogenic protein (BMP) ALK2 receptor (IC50 = 108 nM).- Teresa Rayon, .et al. , Science, 2020, Sep 18;369(6510):eaba7667 PMID: 32943498
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TβRI/II kinase inhibitor
LY2109761, a novel transforming growth factor β receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis- Yimei Wei, .et al. , Int J Rheum Dis, 2024, May;27(5):e15164 PMID: 38706209
- Yan Yang, .et al. , J Thorac Dis, 2024, Feb 29;16(2):1128-1140 PMID: 38505034
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Uto T, .et al. , J Allergy Clin Immunol, 2018, Jun;141(6):2156-2167.e9 PMID: 29477579
- Jared M. Fischer, .et al. , Proc Natl Acad Sci U S A, 2016, Oct 25; 113(43): 12192-12197 PMID: 27791005
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TGF-β/ALK5 inhibitor
A83-01 is a selective inhibitor of the transforming growth factor-beta type I receptor ALK5, the Nodal receptor ALK4, and the nodal receptor ALK7- Yuko Nagashima, .et al. , Sci Rep, 2026, Feb 25;16(1):7582 PMID: 41741551
- T Usui, .et al. , ResearchSquare, 2026, Feb 22
- Jin-Young Lee, .et al. , Mater Today Bio, 2026, Mar 19;38:103026 PMID: 41953717
- Yuko Nagashima, .et al. , Research Square, 2025, Sep 26
- Yuta Shinohara, .et al. , J Vet Med Sci, 2025, Feb 15;87(2):232-240 PMID: 39756955
- Yuko Nagashima, .et al. , Sci Rep, 2025, Feb 19;15(1):6108 PMID: 39972078
- Masayuki Fukumoto, .et al. , PLoS One, 2024, Dec 5;19(12):e0313312 PMID: 39636897
- Raghda Shahin, .et al. , Drug Metabolism and Pharmacokinetics, 2024, 4 December PMID: 40373539
- Kyunghyun Park, .et al. , Advanced Therapeutics, 2024, 7(6)
- Yuko Nagashima, .et al. , Research Square, 2024, June 4th
- Shota Mizuno, .et al. , Biol Pharm Bull, 2024, 47(1):120-129 PMID: 38171772
- Andreea Manole, .et al. , Cell Rep, 2023, Dec 26;42(12):113466 PMID: 38039131
- Claudia Z Han, .et al. , Immunity, 2023, Sep 12;56(9):2152-2171 PMID: 37582369
- Yomogi Shiota Sato, .et al. , Biomed Pharmacother, 2023, Sep;165:115079 PMID: 37413906
- Yomogi Sato, .et al. , Biomed Pharmacother, 2023, Jun;162:114651 PMID: 37030135
- Dan Zhao, .et al. , Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Anna Nakanishi, .et al. , Regen Ther, 2022, Sep 9;21:351-361 PMID: 36161099
- Amira Abugomaa, .et al. , Biomed Pharmacother, 2022, Oct;154:113597 PMID: 36030590
- Isamu Ogawa, .et al. , Biomaterials, 2022, Sep;288:121696 PMID: 36038421
- Mohamed Elbadawy, .et al. , Cancer Biol Ther, 2021, Jun 3;22(5-6):357-371 PMID: 34034619
- Mohamed Elbadawy, .et al. , Authorea, 2020, October 20
- Daichi Onozato, .et al. , Biol Pharm Bull, 2020, 43(7), 1088-1095 PMID: 32612071
- Amira Abugomaa, .et al. , Sci Rep, 2020, Jun 10;10(1):9393 PMID: 32523078
- Jing-Yu Lin, .et al. , Cell Discov, 2020, 6: 20 PMID: 32284878
- Kondo S, .et al. , Biol Open, 2020, Jan 9;9(1) PMID: 31919043
- Onozato D, .et al. , Drug Metab Dispos, 2018, Nov;46(11):1572-1580 PMID: 29615438
- Usui T, .et al. , Curr Protoc Toxicol, 2018, Feb 21;75:22.6.1-22.6.7 PMID: 29512123
- Kondo S, .et al. , Inflamm Res, 2018, Dec;67(11-12):975-984 PMID: 30317465
- Onozato D, .et al. , Stem Cells Dev, 2018, Aug 1;27(15):1033-1045 PMID: 29742964
- Tatsuya Usui, .et al. , Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
- Tatsuya Usui, .et al. , Cancer Sci, 2017, Dec; 108(12): 2383-2392 PMID: 29024204
- Tatsuya Usui, .et al. , Physiol Rep, 2017, Jun; 5(12): e13318 PMID: 28642339
- Tatsuya Usui, .et al. , Stem Cells Int, 2016, 2016: 7053872 PMID: 28119740
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TGF-βR Inhibitor
LY2157299 is an orally active transforming growth factor beta receptor (TGF-βR) kinase inhibitor.- Yuri Nagaoka, .et al. , Arch Biochem Biophys, 2024, Jan:751:109824 PMID: 37984759
- Eunji Jang, .et al. , Exp Mol Med, 2023, May;55(5):974-986 PMID: 37121972
- Satoshi Endo, .et al. , Nutr Res, 2019, 4 November PMID: 31767206
- Oguri G, .et al. , Am J Physiol Heart Circ Physiol., 2014, 307(9):H1339-52 PMID: 25172898
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BMP receptor inhibitor
LDN-212854 is an ALK2-Biased BMP Type I Receptor Kinase Inhibitor. -
Smad inhibitor
Kartogenin potently induces differentiation of human mesenchymal stem cells into chondrocytes -
ALK2 inhibitor
LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM. -
TGFβRI inhibitor
LY 3200882 is a potent, highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). It potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion. -
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. -
TGFβRI kinase inhibitor
TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively. -
Smad2/3 Inhibitor
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. -
Smad3 Inhibitor
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. -
Syk Inhibitor, NF-κB p65 Inhibitor, TGF-β1/Smad Signaling Inhibitor
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. -
TGF-β Inhibitor
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. -
TGF-β1/Smad Signaling Pathway Inhibitor
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. -
TGF-β1 Inhibitory 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. -
TGF-β1 Inhibitor
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. -
TGF-β/Smad/MAPK Inhibitor
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. -
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. -
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. -
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. -
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. -
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.
