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TGF-beta/Smad

The transforming growth factor beta (TGFB) signaling pathway is involved in many cellular processes in both the adult organism and the developing embryo including cell growth, cell differentiation, apoptosis, cellular homeostasis and other cellular functions. In spite of the wide range of cellular processes that the TGFβ signaling pathway regulates, the process is relatively simple. TGFβ superfamily ligands bind to a type II receptor, which recruits and phosphorylates a type I receptor. The type I receptor then phosphorylates receptor-regulated SMADs (R-SMADs) which can now bind the coSMAD SMAD4. R-SMAD/coSMAD complexes accumulate in the nucleus where they act as transcription factors and participate in the regulation of target gene expression.

  • A 83-01
    T3031909910-43-6
    A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12/45/7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.
    • $52
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  • SB-431542
    T1726301836-41-9
    SB-431542 is an inhibitor of ALK5/TGF-β type I Receptor (IC50=94 nM) and is selective. SB 431542 also has inhibitory activity against ALK4 and ALK7 but not other proteins. SB 431542 can be used for induced differentiation of stem cells.
    • $50
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  • Alantolactone
    T2896546-43-0
    Alantolactone (Inula camphor)(Alant camphor), a sesquiterpene lactone, has potential activity against triple-negative breast Y MDA-MB-231 cells by suppressing the signal transducer and activator of transcription 3 (STAT3) signaling pathway.
    • $50
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  • Galunisertib
    T2510700874-72-2
    Galunisertib (LY2157299) is an orally available inhibitor of TGFβRI kinase (IC50: 56 nM) with potential antineoplastic activity.
    • $40
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  • Asiaticoside
    T302516830-15-2
    Asiaticoside (Emdecassol) (Madecassol) is the active chemical component of the plant Centella asiatica. Asiaticoside is used to study potential treatments for wounds and burns.
    • $50
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  • BMT-124110 Formate
    T10572L In house
    BMT-124110 Formate is a selective AAK1 inhibitor (IC50: 0.9 nM) with anti-injury sensory activity.BMT-124110 Formate inhibits the BMP-2-inducible protein kinase BIKE with an IC50: 17 nM.BMT-124110 Formate inhibits the cell-cycle protein G-related BMT-124110 Formate inhibits the cell cycle protein G-associated kinase GAK with an IC50:99 nM.
    • $195
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  • LSKL, Inhibitor of Thrombospondin TSP-1 2TFA
    T7676
    LSKL, Inhibitor of Thrombospondin TSP-1 2TFA is activation of TGF-β .
    • $45
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  • HALOFUGINONE LACTATE
    T878582186-71-8
    HALOFUGINONE LACTATE is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity
    • $55
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  • Disitertide acetate
    T11052L
    Disitertide acetate (P144 acetate) is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide acetate is also a PI3K inhibitor and an apoptosis inducer.
    • $152
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  • Pentabromophenol
    T20319608-71-9
    Pentabromophenol (NSC-5717) suppressed TGF-β response by accelerating the turnover rate of TGF-β receptors.
    • $29
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  • ALK2-IN-2
    T102872254409-25-9In house
    ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) (IC50: 9 nM), inhibiting ALK2 700-fold more than ALK3.
    • $93
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  • GW-6604
    T9947452342-37-9In house
    GW-6604 is an ALK5 inhibitor and shows clear antifibrotic effects resulting in liver function improvement.
    • $30
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  • PF-06952229
    T124331801333-55-0In house
    PF-06952229 is a selective inhibitor of TGFβRI. PF-06952229 can be used in studies about the treatment of solid tumors, specifically metastatic breast cancer.
    • $116
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  • CJJ300
    T624831807631-83-9In house
    CJJ300 is a transforming growth factor-β (TGF-β) inhibitor (IC50 : 5.3 μM).CJJ300 inhibits TGF-β signaling by disrupting the formation of the TGF-β-TβR-I-TβR-II signaling complex.CJJ300 inhibits cell migration.
    • $44
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  • AXL-IN-13
    T733002376928-82-2In house
    AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 value of 1.6 nM and a Kd value of 0.26 nM.AXL-IN-13 exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT) and inhibits cancer cell migration and invasion.
    • $79
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  • Chromenone 1
    T613011639929-29-5In house
    Chromenone 1 is a potent potentiator of osteogenic bone morphogenetic protein (BMP). Chromenone 1 induces a pronounced, kinase-independent, negative TGFβ feedback that enhances nuclear BMP-Smad signaling outputs.
    • $117
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  • Halofuginone hydrobromide
    T352464924-67-0
    Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.
    • $31
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  • LDN-212854
    T19001432597-26-6
    LDN-212854 (BMP Inhibitor III), a novel BMP inhibitor, exhibits greater selectivity for BMP versus the TGF-β type I receptors; possesses differences towards ALK2(IC50=1.3 nM) versus ALK1/3 compared to other inhibitors.
    • $42
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  • SB-505124
    T2462694433-59-5
    SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5.
    • $34
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  • BIX02189
    T24161094614-85-3
    BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.
    • $34
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  • Hydroxysafflor yellow A
    T367478281-02-4
    Hydroxysafflor yellow A (Safflomin A) inhibited adipogenesis by increasing HSL promoter activities. Hydroxysafflor yellow A can effectively protect the liver from long-term alcohol injury by enhancing antioxidant capacity and inhibiting the expression of TGF-β. It prevents steroid-induced avascular necrosis of femoral head by inhibiting primary bone marrow-derived mesenchymal stromal cells. Also, Hydroxysafflor yellow A has anti-tumor effects.
    • $70
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  • LY2109761
    T2123700874-71-1
    LY2109761 is a novel selective TGF-β receptor type I II (TβRI II) dual inhibitor with Ki of 38 nM and 300 nM, respectively; shown to negatively affect the phosphorylation of Smad2.
    • $39
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  • Dorsomorphin dihydrochloride
    T61461219168-18-9
    Dorsomorphin dihydrochloride (BML-275 2HCl) is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.
    • $30
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  • BMP signaling agonist sb4
    T7799100874-08-6
    BMP signaling agonist sb4 (SB 4) is an agonist of benzoxazole bone morphogenetic protein (BMP) signaling (EC50 :74 nM)
    • $39
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  • Oxymatrine
    T275416837-52-8
    Oxymatrine (Oxysophoridine) is an alkaloid isolated from Sophora flavescens, used as the antibiotic. It is a traditional Chinese medicine used in the treatment against hepatitis B virus.It can also inhibit iNOS expression and TGF - β Smad pathway.
    • $41
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  • (E)-SIS3
    T3636521984-48-5
    (E)-SIS3 (SIS3), a selective Smad3 inhibitor, can attenuate TGF-β1-dependent Smad3 phosphorylation and DNA binding. It has no effect on p38 MAPK, Smad2, ERK or PI3K signaling. It also inhibits TGF-β1-induced myofibroblast differentiation of dermal fibroblasts and inhibits TGF-β2-induced endothelial cell differentiation in iPSCs.
    • $36
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  • LY-364947
    T2048396129-53-6
    LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.
    • $59
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  • SB 525334
    T1763356559-20-1
    SB-525334 is a potent and selective inhibitor of the TGF-β1R and ALK5 (IC50: 14.3 nM).
    • $53
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  • Monocrotaline
    T2803315-22-0
    Monocrotaline (Crotaline) is a pyrrolizidine alkaloid and a toxic plant constituent that poisons livestock and humans through the ingestion of contaminated grains and other foods. The alkaloid causes pulmonary artery hypertension, right ventricular hypertrophy, and pathological changes in the pulmonary vasculature. Significant attenuation of the cardiopulmonary changes is noted after oral magnesium treatment.
    • $41
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  • Pirfenidone
    T238653179-13-8
    Pirfenidone (AMR69) is an inhibitor for TGF-β production and TGF-β stimulated collagen production. Pirfenidone inhibits fibroblast, epidermal, platelet-derived, and transforming beta-1 growth factors, thereby slowing tumor cell proliferation. This agent also inhibits DNA synthesis and the production of mRNA for collagen types I and III, resulting in a reduction in radiation-induced fibrosis.
    • $30
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  • Dorsomorphin
    T1977866405-64-3
    Dorsomorphin (BML-275) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy, and possesses antitumor activity.
    • $48
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  • LDN193189
    T19351062368-24-4
    LDN193189 (LDN-193189) (DM 3189) is a selective BMP signaling inhibitor, inhibiting the transcriptional activity of ALK2 and ALK3 (IC50s: 0.8/0.8/5.3/16.7 nM for ALK1/2/3/6).
    • $41
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  • DMH-1
    T19421206711-16-1
    DMH-1 is a potent and selective BMP inhibitor.
    • $53
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  • SRI-011381 hydrochloride
    T51292070014-88-7
    SRI-011381 hydrochloride, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.
    • $39
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  • Vactosertib
    T64961352608-82-2
    Vactosertib (EW-7197) is an orally bioavailable inhibitor of the serine threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity.
    • $39
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  • RepSox
    T6337446859-33-2
    RepSox (ALK5 Inhibitor II) is a TGFβR-1/ALK5 inhibitor that selectively inhibits the binding of ATP to ALK5 and the autophosphorylation of ALK5 (IC50=23/4 nM). RepSox induces adipogenesis in MEFs cells.
    • $30
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  • Hesperetin
    T2565520-33-2
    Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges.
    • $38
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  • BIO-013077-01
    T8330746667-48-1
    BIO-013077-01 is a potent TGFbeta family type I receptors antagonist.
    • $72
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  • DT-6
    T797892414315-95-8
    DT-6, a potent TGF-β1 inhibitor, impedes M2 macrophage-induced epithelial-to-mesenchymal transition and the invasive migration of cancer cells, thereby showing potential for cancer research applications [1].
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  • Myristoyl tetrapeptide-12
    T80628959610-24-3
    Myristoyl Tetrapeptide-12 activates SMAD2 and facilitates the association of SMAD3 with DNA, promoting eyelash hair growth [1] [2].
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  • Ascrinvacumab
    T768581463459-96-2
    Ascrinvacumab (PF-03446962) is a highly humanized IgG2 monoclonal antibody against ALK-1. Ascrinvacumab has a Kd value of 7 nM for human ALK1. Ascrinvacumab has an inhibitory effect on TGF-β and can be used to study hepatocellular carcinoma (HCC).
    • $247
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  • Fresolimumab
    T76681948564-73-6
    Fresolimumab (GC1008) is a specific human anti-transforming growth factor β monoclonal antibody that binds to the active forms of human TGFβ1, TGFβ2, and TGFβ3 and can be used to study focal segmental glomerulosclerosis and cancer in adults.
    • $597
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  • Garetosmab
    T770192097125-54-5
    Garetosmab (REGN 2477) is A whole-human IgG4 monoclonal antibody that selectively inhibits activin A and acts on COVID-19 44. Garetosmab has potential anti-cancer activity and can be used to study ossifying fibrous dysplasia (FOP) and cancer.
    • $328
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  • Carotuximab
    T769411268714-50-6
    Carotuximab (DE-122) is a novel endocholine antibody with strong antiangiogenic and anti-inflammatory activity. Carotuximab blocks endothelial glycoprotein (CD105) and its downstream Smad signaling pathway. Carotuximab has immunomodulatory and antitumor effects to prevent human endothelial dysfunction induced by hypercholesterolemia and hyperglycemia.
    • $247
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  • TGFβ-IN-5
    T77786259870-32-1
    TGFβ-IN-5 (WAY-641966) is a potent TGFβ inhibitor with anti-prion activity for the study of fibroproliferative diseases associated with TGF-β signaling.
    • $52
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  • Nisevokitug
    T805622649854-92-0
    Nisevokitug (NIS-793) is an IgG2λ human monoclonal antibody that targets TGF-β (TGFB1/TGFB2). It is produced in CHO-K1 cells [1].
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  • Elezanumab
    T768631791416-49-3
    Elezanumab(ABT-555) is a potent human anti-RGMa monoclonal antibody.Elezanumab exerts its inhibitory effect on RGMa-mediated BMP signaling through the SMAD1 5 8 pathway, with an IC50 of approximately 97 pM.Elezanumab promotes neuroregeneration, neuroprotection, and neural restoration in models of neuronal injury and demyelination. Elezanumab promotes the growth of corticospinal axons into spinal gray matter and enhances serotonergic innervation in the ventral horn, forming synaptic connections in the caudal part of cervical lesions.
    • $289
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  • Hydrochlorothiazide
    T144958-93-5
    Hydrochlorothiazide (HCTZ) is a Thiazide Diuretic. The physiologic effect of hydrochlorothiazide is by means of Increased Diuresis.
    • $29
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  • (Rac)-SIS3 free base
    T129231009104-85-1
    SIS3 free base is a potent and selective Smad3 phosphorylation inhibitor. SIS3 free base inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.
    • $734
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  • BIBF0775
    T5197334951-90-5
    BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).
    • $60
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