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Pathways Recommended: TGF-beta/Smad
Results for "

TGF-βR1

" in MedChemExpress (MCE) Product Catalog:

11

Inhibitors & Agonists

1

Natural
Products

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-168990
    Ontunisertib

    AGMB-129

    		 TGF-β Receptor Metabolic Disease Inflammation/Immunology Cancer
    Ontunisertib (AGMB-129) is an orally active and selective gastrointestinal-restricted ALK5 (TGFβR1) inhibitor. Ontunisertib blocks signalling of the pro-fibrotic TGFβ pathway. Ontunisertib can be used for the research of fibrostenotic Crohn’s disease .
    Ontunisertib
  • HY-W107024
    BMS-986260

    		TGF-β Receptor Inflammation/Immunology Cancer
    BMS-986260, an immuno-oncology agent, is a potent, selective, and orally active TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC50 of 350 nM and 190 nM, respectively .
    BMS-986260
  • HY-18766
    EW-7195
    1 Publications Verification

    		 TGF-β Receptor p38 MAPK Cancer
    EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung .
    EW-7195
  • HY-160215
    GFH018

    		TGF-β Receptor p38 MAPK TGF-beta/Smad Interleukin Related Cancer
    GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC50 of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma .
    GFH018
  • HY-132290
    TGFβRI-IN-3

    		TGF-β Receptor Inflammation/Immunology Cancer
    TGFβRI-IN-3 inhibits TGFβR1 at an IC50 of 0.79 nM with 2000-fold selectivity against MAP4K4. TGFβRI-IN-3 represents a highly selective TGFβR1 inhibitor that has potential applications in immuno-oncology .
    TGFβRI-IN-3
  • HY-N7694
    Isotoosendanin
    1 Publications Verification

    		 TGF-β Receptor JAK STAT Apoptosis Inflammation/Immunology Cancer
    Isotoosendanin is an orally active TGFβR1 inhibitor and abrogating its kinase activity (IC50 = 6732 nM). Isotoosendanin inhibits the JAK/STAT3 signaling pathway by directly targeting SHP-2, enhancing its stability, and reducing its ubiquitination. Isotoosendanin inhibits TGF-β-induced reduces the migration, invasion, and metastasis in triple-negative breast cancer (TNBC) cells. Isotoosendanin exhibits anti-tumor efficacy in TNBC xenograft models and A549 xenograft tumors. Isotoosendanin exhibits significant anti-inflammatory effects in acetic acid-induced vascular permeability and λ-carrageenan-induced hind paw edema tests. Isotoosendanin can be used for the study of non-small cell lung cancer (NSCLC), TNBC and inflammation .
    Isotoosendanin
  • HY-E70867
    TGFβR2 Recombinant Human Active Protein Kinase

    		TGF-β Receptor Metabolic Disease
    TGF-β is a pleiotropic multifunctional cytokine that regulates many cellular processes, such as cell growth, differentiation, apoptosis and cellular homeostasis. Before exerting the biological effects within cells, TGF-β first requires extracellular activation, namely binds to its type II receptor (TGFβR2) and promotes the phosphorylation. TGFβR1 plays an important role in TGF-β signaling transduction and serves as a tumor suppressor. TGFβR2 Recombinant Human Active Protein Kinase is a recombinant TGFβR2 protein that can be used to study TGFβR2-related functions .
    TGFβR2 Recombinant Human Active Protein Kinase
  • HY-160215A
    GFH018 methylbenzenesulfonate

    		TGF-β Receptor p38 MAPK TGF-beta/Smad Interleukin Related Cancer
    GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC50 of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma .
    GFH018 methylbenzenesulfonate
  • HY-151279
    ALK5-IN-30

    		Anaplastic lymphoma kinase (ALK) Cancer
    ALK5-IN-30 (EX-07) is a potent ALK inhibitor, inhibits ALK5 and TGFβ-R1 with both IC50s <10 nM .
    ALK5-IN-30
  • HY-E70866
    TGFβR1 Recombinant Human Active Protein Kinase

    		TGF-β Receptor Cancer
    TGFβR1 plays an important role in TGF-β signaling transduction and serves as a tumor suppressor. TGFβR1 Recombinant Human Active Protein Kinase is a recombinant TGFβR1 protein that can be used to study TGFβR1-related functions .
    TGFβR1 Recombinant Human Active Protein Kinase
  • HY-149196
    TGFβ-IN-3

    		TGF-β Receptor Cancer
    TGFβ-IN-3 (Compound 8) is a long-acting tumor-activating prodrug of TGFβR1 inhibitor. TGFβ-IN-3 can achieve selective drug release in tumors, and the tumor/blood ratio is increased by 2.2 times. TGFβ-IN-3 can be used for the study of colon cancer .
    TGFβ-IN-3

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