2. Signaling Pathways
  3. TGF-beta/Smad
  4. TGF-β Receptor
  5. TGFβR2 Isoform

TGFβR2

TGFβR2 is the type II TGF-β receptor that initiates signaling after ligand binding and activates TGFβR1/ALK5, which then drives SMAD2/3 transcriptional responses[1]. Mechanistically, TGFβR2 expression levels tune SMAD and MAPK-ERK activation, linking receptor abundance to pathway specificity, p21 induction, and TGF-β-mediated apoptosis[2]. Compared with related TGF-β isoforms, TGF-β2 binds TβRII weakly and depends more on betaglycan, whereas residue differences explain stronger receptor binding by TGF-β1 and TGF-β3[3]. In colorectal cancer, TGFBR2 mononucleotide mutations occur frequently in MSI-high tumors but do not add prognostic value beyond MSI status[4]. In mouse intestinal tumors, epithelial Tgfbr2 loss cooperates with Apc mutation to promote invasion and malignant transformation[5]. For experimental applications, CRISPR/Cas9 TGFBR2 knockout in CAR T cells or ovarian cancer TILs reduces TGF-β immunosuppression and improves antitumor function in TGF-β-rich models[6][7]. A soluble splice variant, TβRII-SE, binds all three TGF-β isoforms and supports fibrosis-model testing of ligand-sequestration strategies[8].- TGFβR2 connects ligand recognition to SMAD2/3 signaling and context-dependent MAPK-ERK activation[1][2]. - TGFBR2 mutation and knockout models support colorectal cancer and immunotherapy mechanism studies[4][5][6][7]. - Isoform-selective binding distinguishes TGF-β2 biology and guides receptor-focused experimental design[3][8].

References:

Cat. No. Product Name Effect Purity
  • HY-117887
    Fidrisertib
    		Inhibitor 98.58%
    Fidrisertib (BLU-782) is the orally active inhibitor for activin receptor-like kinase 2 (ALK2) that inhibits ALK2R206H, ALK2, ALK1, ALK6, ALK3, ALK4, TGFβR2 and ALK5 with IC50s of 0.2, 0.6, 3, 24, 45, 65, 67 and 155 nM, respectively.
  • HY-P990009
    Nisevokitug
    		Inhibitor
    Nisevokitug (NIS-793) is a humanized IgG2λ monoclonal antibody and an inhibitor of the TGF-β signaling pathway. Nisevokitug blocks the binding of TGF-β to the membrane-bound TGF-βR1/TGF-βR2 receptors, inhibits both Smad-dependent and Smad-independent downstream cascade signaling, downregulates fibrosis-related genes, and reverses the TGF-β-mediated immunosuppressive microenvironment. Nisevokitug can be used in the research of diseases such as pancreatic ductal adenocarcinoma, colorectal cancer, myelofibrosis, and myelodysplastic syndrome.
  • HY-161398
    TGFβRII-IN-3
    		Degrader 99.51%
    TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) (IC50 = 4.1 μM). TGFβRII-IN-3 inhibits TGFβ signaling by promoting the proteolytic degradation of TGFβ RII. TGFβRII-IN-3 can block endothelial-to-mesenchymal transition and cell migration. TGFβRII-IN-3 can be used in cancer research.
  • HY-161400
    TGFβRII-IN-2
    		Inhibitor
    TGFβRII-IN-2 (Compound 3n) is an inhibitor for transforming growth factor-β type II receptor (TGFβRII) with IC50 of 2.4 μM, which blocks endothelial-to-mesenchymal transition and cell migration in different cancer cell lines without perturbing the microtubule network.
Cat. No. Product Name / Synonyms Species Source