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

TGF-β Receptor

Transforming growth factor beta receptors

TGF-β Receptor

Related Products

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TGF-β receptors (Transforming growth factor-β receptors) are single pass serine/threonine kinase receptors. Transforming growth factor beta (TGF-beta) is a member of a large family of pleiotropic cytokines that are involved in many biological processes, including growth control, differentiation, migration, cell survival, adhesion, and specification of developmental fate, in both normal and diseased states. TGF-beta superfamily members signal through a receptor complex comprising a type II and type I receptor, both serine/threonine kinases.

The type I receptors, referred to as activin receptor-like kinases (ALK), lie at the epicenter of the signaling cascade as they transduce TGF-beta signals to intracellular regulators of transcription known as Smad proteins. ALKs possess an extracellular binding domain, a transmembrane domain, a GS domain that serves as the site of activation by type II receptors, and a kinase domain that activates downstream signaling molecules. ALKs mediate the effect of TGF-beta superfamily on a variety of cellular processes such as proliferation, differentiation, apoptosis, adhesion and migration, and therefore play important roles in many biological processes. Some ALKs have been implicated in several disorders, including tumorigenesis and immune diseases, suggesting that these receptors can be used as drug targets.

TGF-β Receptor Isoform Specific Products:

TGF-β Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-109179
    Itacnosertib
    		Inhibitor 99.06%
    Itacnosertib (TP-0184) is both inhibitor to JAK2, ACVR1 (ALK2) and ALK5 as described in WO2014151871.
    Itacnosertib
  • HY-122856
    AZ12601011
    		Inhibitor 99.88%
    AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
    AZ12601011
  • HY-145608
    Zilurgisertib
    		Inhibitor 99.77%
    Zilurgisertib (INCB-000928; NBU-928) is a selective ALK 2 inhibitor for researching diseases such as cancer.
    Zilurgisertib
  • HY-141645
    IMM-H007
    		Antagonist
    IMM-H007 (WS070117) is an orally active and potent AMPK (AMP-activated protein kinase) activator and TGFβ1 (transforming growth factor β1) antagonist. IMM-H007 has protective effects in cardiovascular diseases via activation of AMPK. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 degradation. IMM-H007 resolves hepatic steatosis in HFD-fed hamsters by the regulation of lipid metabolism. IMM-H007 can be used for the research of nonalcoholic fatty liver disease (NAFLD) and inflammatory atherosclerosis.
    IMM-H007
  • HY-137506
    XST-14
    		Inhibitor 99.26%
    XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects.
    XST-14
  • HY-112815
    ALK2-IN-2
    		Inhibitor 99.56%
    ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3.
    ALK2-IN-2
  • HY-P99305
    Metelimumab
    		Inhibitor
    Metelimumab (CAT-192) is a human IgG4 monoclonal antibody that can selectively neutralize TGFβ1.
    Metelimumab
  • HY-136773A
    KER047 succinate
    		Inhibitor 98.93%
    ALK2-IN-4 succinate is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base.
    KER047 succinate
  • HY-P2294A
    pm26TGF-β1 peptide TFA
    		99.68%
    pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
    pm26TGF-β1 peptide TFA
  • HY-100434
    PD-161570
    		Inhibitor 99.82%
    PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
    PD-161570
  • HY-136773
    KER047
    		Inhibitor 99.35%
    ALK2-IN-4 is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base.
    KER047
  • HY-W107024
    BMS-986260
    		Inhibitor 98.03%
    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-P99588
    Stamulumab
    		Inhibitor
    Stamulumab (MYO-029) is a recombinant human IgG1λ antibody that binds to myostatin and neutralizes its activity by preventing binding to its endogenous high-affinity receptor ActRIIB. Stamulumab leads to muscle fiber hypertrophy and not hyperplasia in SCID mice. Stamulumab has the potential for Becker muscular dystrophy (BMD), facioscapulohumeral dystrophy (FSHD), and limb-girdle muscular dystrophy (LGMD) research.
    Stamulumab
  • HY-10327
    GW-6604
    		Inhibitor ≥98.0%
    GW-6604 is an ALK5 inhibitor with an IC50 value of 140 nM for inhibiting its autophosphorylation, and can be used in the study of liver fibrosis.
    GW-6604
  • HY-13521A
    SB-505124 hydrochloride
    		Inhibitor 99.34%
    SB-505124 hydrochloride is a selective inhibitor of?TGF-β Receptor type I receptor (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.
    SB-505124 hydrochloride
  • HY-117887
    Fidrisertib
    		Inhibitor
    ALK2-IN-1 is a activin receptor-like kinase-2 (ALK2) inhibitor extracted from patent WO2017181117A1, Compound 876, has an IC50 of <10 nM.
    Fidrisertib
  • HY-154970
    BMPR2-IN-1
    		Inhibitor
    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.
    BMPR2-IN-1
  • HY-150169
    THRX-144644
    		Inhibitor 99.90%
    THRX-144644 is a Lung-restricted ALK5 inhibitor with an IC50 value of 0.14 nM. THRX-144644 avoids systemic toxicities associated with TGFβ pathway inhibition.
    THRX-144644
  • HY-109179A
    Itacnosertib (hydrocholide)
    		Inhibitor 99.43%
    Itacnosertib hydrocholide is an inhibitor of JAK2, ACVR1 (ALK2) and ALK5.
    Itacnosertib (hydrocholide)
  • HY-128437
    TGFβ-IN-5
    		Inhibitor 98.03%
    TGFβ-IN-5(Compd 12) is a TGFβ inhibitor useful for the study of fibroproliferative diseases associated with TGF-β signaling.
    TGFβ-IN-5
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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