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  3. TGF-beta/Smad
  4. TGF-β Receptor

TGF-β Receptor

Transforming growth factor beta receptors

TGF-β Receptor

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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. Nombre del producto Efecto Pureza Chemical Structure
  • HY-128437
    TGFβ-IN-5
    		Inhibitor 98.03%
    TGFβ-IN-5 is a type I transforming growth factor-β receptor (TGF-β R1) kinase inhibitor with an IC50 value of 0.0485 μM. TGFβ-IN-5 reverses the effect of TGF-β-mediated cell activation on the expression of fibrosis-related genes. TGFβ-IN-5 can be used in the research of fibroproliferative diseases.
    TGFβ-IN-5
  • HY-15472
    PRX-08066
    		Inhibitor
    PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 inhibits pulmonary vascular remodeling. PRX-08066 can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET).
    PRX-08066
  • HY-112815
    ALK2-IN-2
    		Inhibitor 99.93%
    ALK2-IN-2 is an orally active and selective inhibitor of ALK2 (ACVR1), with an IC50 value of 9 nM, and over 700-fold selectivity against ALK3. ALK2-IN-2 can inhibit oxidative stress and protect endothelial cells.
    ALK2-IN-2
  • HY-132290
    TGFβRI-IN-3
    		Inhibitor 98.21%
    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-109179
    Itacnosertib
    		Inhibitor 99.06%
    Itacnosertib (TP-0184) is the inhibitor for FLT3, ACVR1 (ALK2, IC50=8 nM) and JAK2 (IC50=8540 nM). Itacnosertib exhibits anti-leukemic activity.
    Itacnosertib
  • HY-W107024
    BMS-986260
    		Inhibitor 99.95%
    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-N5124
    Meloside A
    		Inhibitor 98.72%
    Meloside A (Isovitexin 2''-O-glucoside) is a flavonoid with antioxidant activity. Meloside A can inhibit cell apoptosis and ROS production. Meloside A can inhibit androgen receptor (AR) nuclear translocation and AR protein expression. Meloside A can reduce IL-6, TGF-β1 and DKK-1 levels. Meloside A can be used for the researches of inflammation and endocrinology, such as hair loss.
    Meloside A
  • HY-160215
    GFH018
    		Inhibitor 98.59%
    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-P4651
    H-Tyr-Ile-Gly-Ser-Arg-NH2
    		Inhibitor 98.27%
    H-Tyr-Ile-Gly-Ser-Arg-NH2 is a hexapeptide that is an essential fragment of laminin responsible for efficient cell adhesion and receptor binding. H-Tyr-Ile-Gly-Ser-Arg-NH2 promotes various epithelial cell adhesion activities.
    H-Tyr-Ile-Gly-Ser-Arg-NH2
  • HY-N2589
    Isosaponarin
    		Activator 99.59%
    Isosaponarin is a flavone glycoside isolated from wasabi leaves. Isosaponarin is a P4HA2 enzymatic agonist. Isosaponarin increases collagen synthesis via up-regulated TGF-β type II receptor (TβR-II) and prolyl 4-hydroxylase (P4H) proteins production, promoting skin health and wound healing. Isosaponarin-rich plants exhibit strong antimicrobial, antioxidant, anti-hyaluronidase, antiplatelet, anti-atopic dermatitis, and anti-tumor effects.
    Isosaponarin
  • HY-P0301
    SLLK, Control Peptide for TSP1 Inhibitor
    		Control 99.70%
    SLLK, Control Peptide for TSP1 Inhibitor is a control peptide for LSKL (leucine-serine-lysine-leucine).
    SLLK, Control Peptide for TSP1 Inhibitor
  • HY-B1829AR
    Dexamethasone phosphate disodium (Standard)
    		Inhibitor
    Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium (Standard) is the analytical standard of Dexamethasone phosphate disodium (HY-B1829A). This product is intended for research and analytical applications. Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate disodium is produced by introducing a phosphate ester group at the 21-position of the Dexamethasone molecule, forming a salt with sodium ions, thereby significantly improving water solubility. Dexamethasone phosphate disodium inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate disodium inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate disodium is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate disodium can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease).
    Dexamethasone phosphate disodium (Standard)
  • HY-13521A
    SB-505124 hydrochloride
    		Inhibitor 98.52%
    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-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-N6017
    Bakkenolide A
    		Inhibitor 99.99%
    Bakkenolide A is an anticancer agent. Bakkenolide A reduces the viability of leukemia cells, inhibits cell colony formation and invasion, and downregulates the expression of HDAC3 in cells. Bakkenolide A downregulates the expression of pro-inflammatory cytokines including TNF-α, interleukins such as IL-1β, TGF-β1 and IFN-γ, as well as the expression of PI3K, PDK and PKC in leukemia cells. Bakkenolide A downregulates activated Akt, GSK and Bad, while upregulates Cyto-c, cleaved Caspase3 and cleaved Caspase7, induces apoptosis (apoptosis) in leukemia cells and thereby inhibits inflammatory responses in leukemia cells. Bakkenolide A significantly slows the growth of subcutaneous leukemia tumors in nude mice. Bakkenolide A is applicable to leukemia-related research.
    Bakkenolide A
  • 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-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-125851
    TP-008
    		Inhibitor 99.42%
    TP-008, a chemical probe, is a potent, selective and orally active (Activin-Like Kinase 5) ALK5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.
    TP-008
  • 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-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
Cat. No. Nombre del producto / Synonyms Species Source
Cat. No. Nombre del producto / Synonyms Application Reactivity
TGF-β Receptor Isoform Comparison

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