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

TGF-β Receptor

Transforming growth factor beta receptors

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-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-13783
    BIBF0775
    Inhibitor 99.42%
    BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
    BIBF0775
  • HY-151289
    ALK5-IN-34
    Inhibitor 98.21%
    ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer.
    ALK5-IN-34
  • HY-136773
    KER047
    Inhibitor 99.35%
    KER047 (ALK2-IN-4) is a potent activin receptor-like kinase-2 (ALK2) inhibitor. KER047 can be used for the research of metabolic disease, such as fibrodysplasia ossificans progressiva (FOP).
    KER047
  • HY-P3970D
    KQFK TFA
    Control 99.55%
    KQFK TFA is the TFA salt form of KQFK (HY-P3970C). KQFK TFA is an inactive control of KRFK (HY-P3970). KRFK is a peptide derived from TSP-1 that can activate TGF-β.
    KQFK TFA
  • 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.
    Ontunisertib
  • HY-158203
    BMP agonist 2
    Agonist 99.26%
    BMP agonist 2 (derivative I-9) is a potent bone-inducing cytokine. BMP agonist 2 promotes bone tissue production by increasing the proportion and activity of osteoblasts. BMP agonist 2 promotes osteoblast proliferation and differentiation through the BMP2-ATF4 signaling axis, in which ATF4 is a transcription factor closely related to osteoblast differentiation and bone formation. BMP agonist 2 can be used in the study of senile osteoporosis (SOP).
    BMP agonist 2
  • HY-130437
    p-nitro-Pifithrin-α
    Inhibitor
    p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4]. non-alcoholic fatty liver disease.
    p-nitro-Pifithrin-α
  • HY-P990022
    Prafnosbart
    Inhibitor
    Prafnosbart (DS-6016A) is an IgG1-kappa, anti-ACVR1 (activin A receptor type 1, ACVRLK2, ALK2, ACVR1A, SKR1) humanized monoclonal antibody. Prafnosbart can be used for bone metabolism disorders research.
    Prafnosbart
  • HY-P99746
    Murlentamab
    Inhibitor
    Murlentamab (3C23K; GM102) is a humanized anti-AMHRII antibody. AMHRII is the anti-Müllerian hormone receptor. Murlentama significantly promotes macrophage-mediated antibody-dependent cell-mediated cytotoxicity (ADCC). Murlentama stimulates pro-inflammatory and anti-tumor internal environment, recruits and activates T cells. Murlentama suppresses tumors growth by inducing naïve macrophage orientation and promoting tumor-associated macrophage (TAM) reprogramming.
    Murlentamab
  • 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-12273R
    DMH-1 (Standard)
    Inhibitor
    DMH-1 (Standard) is the analytical standard of DMH-1. 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.
    DMH-1 (Standard)
  • HY-160215
    GFH018
    Inhibitor
    GFH018 is a TGF-βRI inhibitor. GFH018 can be used for cancer research.
    GFH018
  • HY-P99818
    Ramatercept
    Antagonist ≥99.0%
    Ramatercept (ACE-031) is a soluble ActRIIB receptor and can be used as a soluble activin receptor 2 (ACVR2) antagonist. Ramatercept inhibits the signal pathway of muscle growth inhibition and has potential application in muscle atrophy.
    Ramatercept
  • HY-10432R
    A 83-01 (Standard)
    Inhibitor
    A 83-01 (Standard) is the analytical standard of A 83-01 (HY-10432). This product is intended for research and analytical applications. A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
    A 83-01 (Standard)
  • HY-160237
    HYL001
    Inhibitor 99.94%
    HYL001 (compund 338) is a potent inhibitor of TGFβ receptor 1 (ALK5) that is approximately 9 times more potent than the structurally related compound Galunisertib (HY-13226) and is able to eliminate liver metastases established in mice.
    HYL001
  • HY-118810
    BIO-013077-01
    Inhibitor 99.63%
    BIO-013077-01 is a pyrazole TGF-β inhibitor.
    BIO-013077-01
  • HY-10591
    Neuropathiazol
    98.73%
    Neuropathiazol, a neuronal differentiation inducer, selectively induces neuronal differentiation of multipotent hippocampal neural progenitor cells.
    Neuropathiazol
  • HY-W028145
    TGF-βRI inhibitor 2
    Inhibitor 98.32%
    TGF-βRI inhibitor 2 (compound 13) is a TGF-βRI inhibitor. TGF-βRI inhibitor 2 can be used in cancer research.
    TGF-βRI inhibitor 2
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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