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

TGF-β Receptor Inhibitor

TGF-β Receptor Inhibitors (105):

Cat. No. Product Name Effect Purity
  • HY-13226
    Galunisertib
    		Inhibitor 99.95%
    Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
  • HY-12273
    DMH-1
    		Inhibitor 99.95%
    DMH-1 is a potent and selective BMP inhibitor with IC50s of 27/107.9/<5/47.6 nM for ALK1/ALK2/ALK3/ALK6, respectively.
  • HY-12043
    SB 525334
    		Inhibitor 99.97%
    SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.
  • HY-12075
    LY2109761
    		Inhibitor 99.72%
    LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
  • HY-12071B
    LDN-193189 dihydrochloride
    		Inhibitor 99.75%
    LDN-193189 (dihydrochloride) is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.
  • HY-168990
    Ontunisertib
    		Inhibitor
    Ontunisertib (Example 26) is an inhibitor of TGFβ receptor I/ALK5 (TGFβRI/ALK5), with IC50 values ranging from 100 to 500 nM for TGFβRI and an IC50 value of ≤100 nM for ALK5. Ontunisertib can be used in research on gastrointestinal diseases, as well as diseases and cancers related to fibrotic conditions in the skin and eyes.
  • HY-P991254
    VPI-2690B
    		Inhibitor
    VPI-2690B is a human monoclonal antibody (mAb) targeting Integrin aVb3. VPI-2690B inhibits TGF-β signaling. VPI-2690B can be used in Diabetic nephropathies research.
  • HY-13521
    SB-505124
    		Inhibitor 99.73%
    SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
  • HY-13462
    LY-364947
    		Inhibitor 99.14%
    LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.
  • HY-13227
    SD-208
    		Inhibitor 99.87%
    SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
  • HY-10326
    GW788388
    		Inhibitor 99.92%
    GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
  • HY-N1472
    Levistolide A
    		Inhibitor 99.34%
    Levistolide A is an apoptosis inducer and a PEDV virus inhibitor. Levistolide A can induce apoptosis in colon cancer cells and suppress the replication of porcine epidemic diarrhea virus (PEDV) by promoting ROS generation. Levistolide A activates peroxisome proliferator-activated receptor γ (PPARγ) in N2a/APP695swe cells and reduces excessive phosphorylation of tau through the GSK3α/β pathway, improving symptoms in Alzheimer’s mice. Levistolide A improves kidney damage in 5/6 nephrectomy (Nx) mice by inhibiting the RAS,TGF-β1/Smad, and MAPK pathways.
  • HY-12704
    ITD-1
    		Inhibitor 99.41%
    ITD-1 is the first selective TGFβ receptor inhibitor with an IC50 of 460 nM.
  • HY-12278
    K02288
    		Inhibitor 99.65%
    K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC50s of of 5-34 nM.
  • HY-P99632
    Garetosmab
    		Inhibitor 99.57%
    Garetosmab (REGN 2477) is a fully human IgG4 monoclonal antibody that specifically inhibits activin A. Garetosmab can be used for fibrodysplasia ossificans progressiva (FOP) research.
  • HY-103021
    LY3200882
    		Inhibitor 99.87%
    LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.
  • HY-136244
    PF-06952229
    		Inhibitor 99.92%
    PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction.?PF-06952229 is a promising antineoplastic?agent for the study solid tumors, especifically metastatic breast cancer.
  • HY-154970A
    BMPR2-IN-1 TFA
    		Inhibitor 99.40%
    BMPR2-IN-1 (Compound 8a) is a BMPR2 inhibitor with an IC50 of 506 nM and a KD of 83.5 nM. BMPR2-IN-1 can be used for research of pulmonary arterial hypertension, Alzheimer’s disease and cancer.
  • HY-151427
    TGFβ1-IN-1
    		Inhibitor 99.47%
    TGFβ1-IN-1 (compound 42) is a potent, orally active TGF-β1 inhibitor. TGFβ1-IN-1 inhibits the upregulation of TGF-β1-induced fibrosis markers (α-SMA and fibronectin) and can be used in liver fibrosis disease studies.
  • HY-P99590A
    Sotatercept (mIgG2a)
    		Inhibitor 99.71%
    Sotatercept (mIgG2a) (RAP-011), the murine homolog of Sotatercept (ACE-011) (HY-P99590), is a soluble activin receptor type IIA (ActRIIA) ligand trap. Sotatercept (mIgG2a) inhibits the binding of activin A and other members of the TGF-β superfamily (such as Activin A/B, GDF11 and BMP9/10) to their receptors by combining and neutralizing them, thereby regulating cell proliferation and differentiation. Sotatercept (mIgG2a) mainly inhibits the SMAD2/3 signaling pathway, and can be used in various diseases such as chronic kidney disease. Sotatercept (mIgG2a) reduces the expression of erythropoietic hepcidin (ERFE), regulates iron metabolism, and promotes red blood cell production. Sotatercept (mIgG2a) has a dual effect of promoting bone formation (anabolic) and inhibiting bone resorption (catabolic).