2. Signaling Pathways
  3. Stem Cell/Wnt
    TGF-beta/Smad
  4. TGF-beta/Smad

TGF-beta/Smad

Transforming growth factor beta

TGF-beta/Smad

Related Products

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Transforming growth factor-beta (TGF-β) is a member of a superfamily of pleiotropic proteins that regulate multiple cellular processes such as growth, development and differentiation. The intracellular effectors of TGF-beta signalling, the Smad proteins, are activated by receptors and translocate into the nucleus, where they regulate transcription. Although this pathway is inherently simple, combinatorial interactions in the heteromeric receptor and Smad complexes, receptor-interacting and Smad-interacting proteins, and cooperation with sequence-specific transcription factors allow substantial versatility and diversification of TGF-beta family responses. Other signalling pathways further regulate Smad activation and function.

In addition, TGF-beta receptors activate Smad-independent pathways that not only regulate Smad signalling, but also allow Smad-independent TGF-beta responses. Aberrant TGF-β signaling is associated with a variety of diseases, such as fibrosis, cardiovascular disease and cancer. Hence, the TGF-β signaling pathway is recognized as a potential drug target.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12953
    R-268712
    		Inhibitor 99.92%
    R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer.
    R-268712
  • HY-124447
    BTYNB
    		Inhibitor 98.0%
    BTYNB is a structure-specific nucleic acid binder and IGF2BP1 inhibitor (with an IC50 of 5 μM against hBTYNB). BTYNB disrupts the IGF2BP1-RNA interaction and blocks its binding to oncogenic mRNAs such as c-Myc, MDM2, PD-L1. BTYNB completely blocks the INHBA-Smad2/3 pathway, disrupts the MYCN/IGF2BP1 loop, and thereby induces apoptosis and cell cycle arrest, effectively inhibiting the proliferation and survival of cancer cells. In addition, BTYNB acts as an immune activator and tumor microenvironment modulator, enhances T cell-mediated tumor killing, and produces significant synergistic effects with inhibitors of PD-1, BRD and BIRC5. BTYNB can be used in relevant research on various malignant tumors including ovarian cancer, neuroblastoma, leukemia and melanoma.
    BTYNB
  • HY-118119
    CAY10526
    		Inhibitor 99.12%
    CAY10526 is an inhibitor of Y-box binding protein 1 (YB-1) and microsomal prostaglandin E2 synthase 1 (mPGES1). CAY10526 inhibits the production of PGE2 by suppressing YB-1 and mPGES1. CAY10526 induces cell apoptosis (apoptosis) and inhibits the JAK/STAT, TGF-β/Smad3 and PI3K/AKT signaling pathways. CAY10526 can be used in research related to melanoma, prostate cancer, esophageal adenocarcinoma, T-cell lymphoma, etc.
    CAY10526
  • HY-N2995
    Poricoic acid A
    		Inhibitor 99.19%
    Poricoic acid A can be isolated from Poria cocos. Poricoic acid A is an orally active anti-tumor agent. Poricoic acid A enhances melatonin inhibition of AKI-to-CKD transition by regulating Gas6/AxlNFκB/Nrf2 axis. Poricoic acid A also attenuatea fibroblast activation and abnormal extracellular matrix remodeling in renal fibrosis by activating AMPK and inhibiting Smad3. Poricoic acid A significantly reduces the magnitude of rise in serum creatinine and urea levels in rat model when combined with Melatonin. Poricoic acid A ameliorates renal fibrosis and podocyte injury by attenuating oxidative stress and inflammation through regulating NF-κB and Nrf2 in IRI rodent model in combination with Melatonin.
    Poricoic acid A
  • HY-100438
    Hydronidone
    		Inhibitor 99.71%
    Hydronidone is an orally active pyridine derivative. Hydronidone is an inhibitor of phosphodiesterase-4 (PDE4) and cyclo-oxygenase (COX) as well as TGF-β. Hydronidone induces mitochondrial dysfunction and triggers apoptosis. Hydronidone can be used for liver fibrosis, anti-inflammation and anti-cancer study.
    Hydronidone
  • HY-14928
    Lobeglitazone
    		Inhibitor
    Lobeglitazone is a new type of thiazolidinedione. Lobeglitazone is the orally active agonist for PPAR with EC50 of 137.4 nM and 546.3 nM for PPARγ and PPARα. Lobeglitazone is the inhibitor for ERK/JNK/Smad/NF-κB signaling pathway. Lobeglitazone exhibits anti-inflammatory, anti-diabetic, anti-fibrotic and anti-atherosclerotic properties.
    Lobeglitazone
  • HY-W011121
    2-Oleoylglycerol
    		Activator 99.9%
    2-Oleoylglycerol (2-OG) is a lipid found in the diet. It is a GPR119 agonist, with an EC50 value of 2.5 μM in activating hGPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol enhances the inflammatory response of macrophages and promotes fibrosis by activating the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. It also stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. 2-Oleoylglycerol is expected to be used in the research of non-alcoholic steatohepatitis (NASH) .
    2-Oleoylglycerol
  • HY-P99370
    Landogrozumab
    		Inhibitor 99.79%
    Landogrozumab (LY2495655) is an humanized anti-myostatin monoclonal antibody. Landogrozumab effectively improves muscle volume, hand grip strength and function. Landogrozumab can be used for the research of muscle wasting disease.
    Landogrozumab
  • HY-N0732
    Jolkinolide B
    		Inhibitor 99.65%
    Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud with oral activity. Jolkinolide B downregulates XIAP, cIAP1, cIAP2, and phosphorylated Akt, upregulates Smac, activates caspase-3 and caspase-9, and inhibits NF-κB, TGFβ/smad3 and JAK/STAT3 pathways. Jolkinolide B exerts comprehensive biological effects including inducing cancer cell apoptosis, suppressing inflammatory responses, improving lung function, alleviating hepatic steatosis and eliminating intracellular Mycobacterium tuberculosis. Jolkinolide B can be used for the research of leukemia, histiocytic lymphoma, asthma, metabolic dysfunction-associated steatotic liver disease and tuberculosis.
    Jolkinolide B
  • HY-N0559
    Kirenol
    		Inhibitor 99.82%
    Kirenol is a diterpenoid compound, an orally active apoptosis inducer and signaling pathway regulator, with a Kd value of 5.47 μM against the target CK2. Kirenol promotes the cleavage of Bid into tBid, regulates the protein levels/phosphorylation of Bax, Bcl-2, p53 and p21, and induces caspase-independent apoptosis, S-phase cell cycle arrest, ROS accumulation and cytotoxicity in cancer cells. Kirenol activates the CK2/AKT and AMPK-mTOR-ULK1 pathways, inhibits the signaling of NF-κB, TGF-β/Smads and NLRP3 inflammasome, and regulates the GSK3β, BMP and Wnt/β-catenin pathways. Kirenol induces autophagy, mitophagy and osteoblast differentiation, promotes mitochondrial fusion, and exerts antioxidant, anti-inflammatory, antifibrotic, renoprotective, cardioprotective, neuroprotective and analgesic effects. Kirenol is applicable to research related to chronic myeloid leukemia, ischemic stroke, diabetic nephropathy, heart failure, acute lung injury and osteoporosis.
    Kirenol
  • HY-P991504
    LAE-102
    		Antagonist 99.46%
    LAE-102 is the selective anti-ActRIIA (activin receptor type IIA or ACVR2) monoclonal antibody. LAE-102 increases muscle mass and reduces fat mass. LAE102 can increase serum activin A levels in vivo. LAE-102 is promising for research of obesity.
    LAE-102
  • HY-N6013
    Aloin (mixture of A&B)
    		Inhibitor 99.36%
    Aloin (mixture of A&B) is an orally active anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) mitigates airway impairment and exerts neuroprotective, anti-inflammatory, antioxidant, antibacterial, antifungal, antiviral and antitumor effects. Aloin (mixture of A&B) inhibits Clostridium histolyticum collagenase, granulocyte matrix metalloproteinases and human 20S proteasome. Aloin (mixture of A&B) upregulates the Nrf2/HO-1 pathway, suppresses the TGF-β/Smad2/3 pathway. Aloin (mixture of A&B) reduces IL-4/IL-5/IL-13 levels, and reverses oxidative stress markers (MDA, SOD, GSH). Aloin (mixture of A&B) can be used for research on chronic ulcers, burns, wounds, inflammatory and degenerative disorders, asthma and neuroblastoma.
    Aloin (mixture of A&B)
  • HY-163536
    TGF-β1/Smad3-IN-1
    		Inhibitor 98.05%
    TGF-β1/Smad3-IN-1 (Compound 5aa) is an inhibitor of the TGF-β1/Smad3 signaling pathway(IC50=1.07 μM). TGF-β1/Smad3-IN-1 possesses antifibrotic activity and oral potency.
    TGF-β1/Smad3-IN-1
  • HY-145721A
    Mongersen sodium
    		99.61%
    Mongersen sodium is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen sodium restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen sodium can attenuate Crohn's disease-like experimental colitis in mice.
    Mongersen sodium
  • HY-P99708
    Livmoniplimab
    		Inhibitor 99.25%
    Livmoniplimab (ABBV-151) is a monoclonal antibody against GARP/TGF-β1 that can inhibit the release of active TGF-β1. Livmoniplimab has anti-tumor activity in colon cancer mice. Livmoniplimab can be used for the study of locally advanced or metastatic solid tumors.
    Livmoniplimab
  • HY-B0673R
    Pirfenidone (Standard)
    		Inhibitor
    Pirfenidone (Standard) is the analytical standard of Pirfenidone. This product is intended for research and analytical applications. Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities.
    Pirfenidone (Standard)
  • HY-100534
    IDE 2
    		Agonist 99.00%
    IDE2 is a small molecule cell-permeable inducer of definitive endoderm formation in mouse and human embryonic stem cells (ESCs) by activating the TGF-βsignaling pathway.
    IDE 2
  • HY-107802
    Breviscapine
    		Modulator 99.13%
    Breviscapine (Breviscapinun) is a flavonoid compound with antioxidant, anti-inflammatory, anti-fibrotic, and neuroprotective activities. Breviscapine ameliorates cerebral ischemia/reperfusion injury and vascular dementia, and inhibits the formation of postoperative abdominal adhesions. The mechanism of action of Breviscapine involves the regulation of oxidative stress, inflammatory cytokines, signaling pathways such as TGF-β/Smad, and cellular calcium overload. Breviscapine is used for research on diseases including cardiovascular and cerebrovascular diseases.
    Breviscapine
  • HY-N0657
    Pinoresinol Diglucoside
    		99.84%
    Pinoresinol Diglucoside is an orally active lignan with multifunctional bioactivity. Pinoresinol Diglucoside interacts with targets including ALB, HIF1A, GSK3B, BCL2, MARK3, IL6, NF-κB p65, Nrf2, HO-1, and TLR4, and modulates pathways including PI3K-Akt, estrogen, MAPK, Rap1, AKT/mTOR/NF-κB, and TGF-β1/Smads. Pinoresinol Diglucoside regulates osteogenesis, bone resorption, oxidative stress, inflammation, apoptosis, ferroptosis, ferritinophagy, cardiac fibrosis, and vasorelaxation. Pinoresinol Diglucoside can be used for the research of osteoporosis, ischemia/reperfusion-induced brain injury, Alzheimer’s disease, myocardial ischemia-reperfusion injury, chondrodysplasia, diabetic cardiomyopathy, cardiac hypertrophy, hypertension, cisplatin-induced hearing loss, atherosclerotic cardiovascular diseases, and disuse osteoporosis.
    Pinoresinol Diglucoside
  • HY-132187
    Sphingosylphosphorylcholine
    		Inducer 99.50%
    Sphingosylphosphorylcholine is a bioactive lipid and a major component of plasma high-density lipoprotein that binds to OGR1 with a Kd of 33.3 nM. Sphingosylphosphorylcholine triggers delayed phosphorylation of Smad2, upregulates α-SMA expression, and activates TRPM3. Sphingosylphosphorylcholine reduces Apoptosis and upregulates the expression of uPA and its receptor uPA-R. Sphingosylphosphorylcholine exerts anti-apoptotic, anti-cardiac hypertrophy and pro-wound healing effects. Sphingosylphosphorylcholine induces scratching behavior in mice. Sphingosylphosphorylcholine is used in studies related to atopic dermatitis, promyelocytic leukemia, heart failure, myocardial ischemia/reperfusion injury, ovarian cancer, breast cancer, pancreatic cancer, and skin wound healing disorders in genetically impaired healing diabetes.
    Sphingosylphosphorylcholine
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Cat. No. Product Name / Synonyms Application Reactivity