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Results for "

tgf-beta-t??rs

" in MCE Product Catalog:

92

Inhibitors & Agonists

7

Screening Libraries

6

Peptides

14

Natural
Products

73

Recombinant Proteins

7

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-P2294
    pm26TGF-β1 peptide

    TGF-β Receptor Inflammation/Immunology
    pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
  • HY-P2294A
    pm26TGF-β1 peptide TFA

    TGF-β Receptor Inflammation/Immunology
    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.
  • HY-114192
    TGFβRI-IN-1

    TGF-β Receptor Cancer
    TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively .
  • HY-139858
    TGFβR-IN-1

    TGF-β Receptor Cancer
    TGFβR-IN-1 is a long-acting tumor-activated prodrug of a TGFβR inhibitor.
  • HY-132290
    TGFβRI-IN-3

    TGF-β Receptor Cancer Inflammation/Immunology
    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.
  • HY-146780
    TGFβRI-IN-4

    TGF-β Receptor Cancer
    TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model.
  • HY-N0439
    Asiaticoside

    TGF-beta/Smad Reactive Oxygen Species Apoptosis Endogenous Metabolite Inflammation/Immunology Neurological Disease Cardiovascular Disease Cancer
    Asiaticoside, a trisaccaride triterpene from Centella asiatica, suppresses TGF-β/Smad signaling through inducing Smad7 and inhibiting TGF-βRI and TGF-βRII in keloid fibroblasts; Asiaticoside shows antioxidant, anti-inflammatory, and anti-ulcer properties.
  • HY-13226
    Galunisertib

    LY2157299

    TGF-β Receptor Cancer
    Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
  • HY-146693
    CJJ300

    TGF-β Receptor Cancer
    CJJ300 is a transforming growth factor-β (TGF-β) inhibitor with an IC50 of 5.3 µM. CJJ300 inhibits TGF-β signaling by disrupting the formation of the TGF-β-TβR-I-TβR-II signaling complex.
  • HY-P99020
    Fresolimumab

    GC1008

    TGF-β Receptor Cancer Inflammation/Immunology
    Fresolimumab (GC1008) is a high-affinity fully human monoclonal antibody that neutralizes the active form of human TGFβ1, TGFβ2, and TGFβ3. Fresolimumab can be used for the research of cancer and fibrotic diseases .
  • HY-146434
    TGFβ-IN-2

    TGF-beta/Smad Inflammation/Immunology
    TGFβ-IN-2 (Compound 9d) inhibits TGF-β-induced total collagen accumulation in NRK-49F cells with the IC50 of 4.31 μM. TGFβ-IN-2 suppresses the TGF-β-induced protein expression of COL1A1, α-SMA, and p-Smad3 in vitro. TGFβ-IN-2 can be used as a potential effective compound for anti-fibrosis in vivo by oral administration.
  • HY-147786
    TGFβRI-IN-5

    TGF-β Receptor Cancer
    TGFβRI-IN-5 (Compound 4b) is a potent inhibitor of TGFβRI with an IC50 of 0.08 μM. TGFβRI-IN-5 displays amazing anticancer activity 5–7 times that of reference drug against all the tested cell lines. TGFβRI-IN-5 enhances apoptosis and arrested G2/M phase of cell cycle.
  • HY-13227
    SD-208

    TGF-β Receptor Cancer
    SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
  • HY-13462
    LY-364947

    HTS466284

    TGF-β Receptor Cancer
    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-W107024
    BMS-986260

    TGF-β Receptor Cancer Inflammation/Immunology
    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.
  • HY-118810
    BIO-013077-01

    TGF-β Receptor Cancer
    BIO-013077-01 is a pyrazole TGF-β inhibitor.
  • HY-12704
    ITD-1

    TGF-β Receptor Cardiovascular Disease
    ITD-1 is the first selective TGFβ receptor inhibitor with an IC50 of 460 nM.
  • HY-144043
    ALK5-IN-8

    TGF-β Receptor Cancer
    ALK5-IN-8 is a potent inhibitor of TGFβRI (ALK5). ALK5-IN-8 Inhibits the phosphorylation of ALK5 on its downstream signaling proteins (Smad2 or Smad3) by blocking the binding of TGFβRI to ligands, thereby affecting or blocking TGF-β signaling. ALK5-IN-8 has the potential for the research of various ALK5-mediated related diseases (extracted from patent WO2021190425A1, compound 1).
  • HY-101275
    EMT inhibitor-1

    Hippo (MST) TGF-beta/Smad Wnt Cancer
    EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.
  • HY-100347A
    SRI-011381 hydrochloride

    TGF-beta/Smad Neurological Disease
    SRI-011381 hydrochloride is an orally active TGF-β signaling agonist, exhibits neuroprotective effects.
  • HY-100347
    SRI-011381

    TGF-beta/Smad Neurological Disease
    SRI-011381 is an orally active TGF-β signaling agonist, exhibits neuroprotective effects.
  • HY-12075
    LY2109761

    TGF-β Receptor Autophagy Cancer
    LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
  • HY-N6896
    Isoviolanthin

    TGF-beta/Smad Cancer
    Isoviolanthin, a flavonoid glycoside, could markedly inhibit TGF-β1-mediated migration and invasion by deactivating epithelial-mesenchymal transition (EMT) via the TGF-β/Smad and PI3K/Akt/mTOR pathways in HCC cells. Isoviolanthin exhibits no cytotoxic effects on normal liver LO2 cells.
  • HY-142967
    TGFβ-IN-1

    TGF-β Receptor Cancer
    TGFβ-IN-1 is an antitumor growth and metastasis agent through inhibiting the transforming growth factor‑β signaling pathway.
  • HY-13783
    BIBF0775

    TGF-β Receptor Cancer
    BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
  • HY-18766
    EW-7195

    TGF-β Receptor p38 MAPK Cancer
    EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung.
  • HY-P0299
    LSKL, Inhibitor of Thrombospondin (TSP-1)

    TGF-β Receptor Cancer
    LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier.
  • HY-P0299A
    LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)

    TGF-β Receptor Cancer
    LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier.
  • HY-10431
    SB-431542

    TGF-β Receptor Cancer
    SB-431542 is a potent and selective inhibitor of ALK5/TGF-β type I Receptor with an IC50 value of 94 nM.
  • HY-123900
    AZ12799734

    TGF-β Receptor Cardiovascular Disease
    AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor.
  • HY-13012
    RepSox

    E-616452; SJN 2511

    TGF-β Receptor Cancer
    RepSox (E-616452) is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with an IC50 of 4 nM.
  • HY-112331
    SJ000291942

    TGF-β Receptor Cancer
    SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules.
  • HY-100534
    IDE 2

    TGF-beta/Smad Others
    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.
  • HY-N10438
    Ganodermaones B

    Integrin Inflammation/Immunology
    Ganodermaones B (Compound 2) is a renal fibrosis inhibitor. Ganodermaones B inhibits TGF-β1-induced collagen I and fibronectin expression.
  • HY-78349
    A 77-01

    TGF-β Receptor Cancer
    A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.
  • HY-115669
    Pentachloropseudilin

    Antibiotic A 15104 Y; PClP

    Myosin TGF-β Receptor Cancer
    Pentachloropseudilin (Antibiotic A 15104 Y; PClP) is a reversible and allosteric potent inhibitor of Myo1s (class 1 myosins) with IC50s range from 1 to 5 μM for mammalian class-1 myosins and greater than 90 μM for class-2 and class-5 myosins. Pentachloropseudilin is a potent inhibitor of transforming growth factor-β (TGF-β)-stimulated signaling, with an IC50 of 0.1 to 0.2 μM for TGF-β.
  • HY-142949
    ALK5-IN-7

    ALK Cancer Inflammation/Immunology
    ALK5-IN-7 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-7 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 4).
  • HY-142950
    ALK5-IN-6

    ALK Cancer Inflammation/Immunology
    ALK5-IN-6 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-6 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 1).
  • HY-10326
    GW788388

    TGF-β Receptor Cancer
    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-N0847
    Micheliolide

    NF-κB Others
    Micheliolide could effectively attenuate the high glucose-stimulated activation of NF-κB, the degradation of IκBα, and the expression of MCP-1, TGF-β1 and FN in rat mesangial cells (MCs).
  • HY-13013
    (E)-SIS3

    TGF-beta/Smad Inflammation/Immunology
    (E)-SIS3 is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation. (E)-SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.
  • HY-143891
    Chromenone 1

    TGF-β Receptor Others
    Chromenone 1 is a potent osteogenic bone morphogenetic protein (BMP) potentiator. Chromenone 1 exhibits a unique mode of action as it induces a pronounced, kinase-independent, negative TGFβ feedback that enhances nuclear BMP-Smad signaling outputs.
  • HY-111253
    CYM-5478

    LPL Receptor Neurological Disease
    CYM-5478 is a potent and highly selective S1P2 agonist with an EC50 of 119 nM in a TGFα-shedding assay. CYM-5478 protects neural-derived cell lines against Cisplatin toxicity.
  • HY-N6679A
    10,11-Dehydrocurvularin

    HSP TGF-beta/Smad Cancer Infection
    10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity.
  • HY-114495
    Caerulomycin A

    Cerulomycin; Caerulomycin

    Fungal Antibiotic Infection Inflammation/Immunology
    Caerulomycin A (Cerulomycin; Caerulomycin), an antifungal compound, induces generation of T cells, enhances TGF-β-Smad3 protein signaling via suppressing interferon-γ-induced STAT1 signaling. Antifungal and antibiotic activity, and used in autoimmune diseases.
  • HY-N2589
    Isosaponarin

    TGF-β Receptor Others
    Isosaponarin is a flavone glycoside isolated from wasabi leaves. Isosaponarin increases collagen synthesis, caused by up-regulated TGF-β type II receptor (TβR-II) and prolyl 4-hydroxylase (P4H) proteins production.
  • HY-100608
    BMS453

    BMS-189453

    RAR/RXR Cancer
    BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.
  • HY-100444
    SIS3 free base

    TGF-beta/Smad Inflammation/Immunology
    SIS3 free base is a potent and selective inhibitor of Smad3 phosphorylation. SIS3 free base inhibits the myofibroblast differentiation of fibroblasts by TGF-β1. SIS3 free base does not affect the phosphorylation of Smad2.
  • HY-10432A
    A 83-01 sodium

    TGF-β Receptor Cancer
    A 83-01 sodium is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
  • HY-15897
    LDN-212854

    TGF-β Receptor Cancer
    LDN-212854 is a novel BMP inhibitor that exhibits substantially greater selectivity for BMP versus the TGF-β type I receptors; possesses a bias towards ALK2(IC50=1.3 nM) versus ALK1 and ALK3 compared to other inhibitors.
  • HY-145721
    Mongersen

    GED-0301

    TGF-beta/Smad Inflammation/Immunology
    Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen can attenuate Crohn's disease-like experimental colitis in mice.
  • HY-103021
    LY3200882

    TGF-β Receptor Cancer Inflammation/Immunology
    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-N0158
    Oxymatrine

    TGF-beta/Smad Influenza Virus Cancer Infection Inflammation/Immunology
    Oxymatrine, an alkaloid from the roots of Sophora species, with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and TGF-β/Smad pathway. Oxymatrine inhibits bocavirus minute virus of canines (MVC) replication, reduces viral gene expression and decreases apoptosis induced by viral infection.
  • HY-P0118
    Disitertide

    P144

    TGF-beta/Smad PI3K Apoptosis Cancer
    Disitertide (P144) is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) is also a PI3K inhibitor and an apoptosis inducer.
  • HY-125851
    TP-008

    ALK Inflammation/Immunology
    TP-008 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.
  • HY-B0449
    Methacycline hydrochloride

    Bacterial Antibiotic Infection
    Methacycline hydrochloride is a tetracycline antibiotic and can inhibits bacterial protein synthesis. Methacycline hydrochloride is a potent epithelial-mesenchymal transition (EMT) inhibitor. Methacycline hydrochloride blocks EMT in vitro and fibrogenesis in vivo without directly affecting TGF-β1 Smad signaling. Methacycline hydrochloride is an antimicrobial and has the potential for pulmonary fibrosis.
  • HY-13521
    SB-505124

    TGF-β Receptor Cancer
    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-B0252
    Hydrochlorothiazide

    HCTZ

    TGF-beta/Smad Potassium Channel Metabolic Disease Cardiovascular Disease
    Hydrochlorothiazide (HCTZ), an orally active diuretic drug of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.
  • HY-B0673
    Pirfenidone

    AMR69

    TGF-beta/Smad CCR Inflammation/Immunology Cancer
    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.
  • HY-P0118A
    Disitertide TFA

    P144 TFA

    TGF-beta/Smad PI3K Apoptosis Cancer
    Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) TFA is also a PI3K inhibitor and an apoptosis inducer.
  • HY-13521A
    SB-505124 hydrochloride

    TGF-β Receptor Cancer
    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.
  • HY-124748A
    ENMD-1068 hydrochloride

    Protease Activated Receptor (PAR) Inflammation/Immunology Cardiovascular Disease
    ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist with antiangiogenic and anti-inflammatory activities. ENMD-1068 hydrochloride reduces epatic stellate cells (HSCs) activation and collagen expression through the inhibiton of TGF-β1/Smad signal transduction.
  • HY-100448A
    Butaprost

    Prostaglandin Receptor TGF-beta/Smad Endocrinology
    Butaprost is a selective prostaglandin E receptor (EP2) agonist with an EC50 of 33 nM and a Ki of 2.4 μM for murine EP2 receptor. Butaprost is less activity against murine EP1, EP3 and EP4 receptors. Butaprost attenuates fibrosis by hampering TGF-β/Smad2 signalling.
  • HY-10432
    A 83-01

    TGF-β Receptor Cancer
    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.
  • HY-77251
    TAK1/MAP4K2 inhibitor 1

    MAP4K MAP3K Cancer
    TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
  • HY-N0587
    Demethylzeylasteral

    Apoptosis Cancer Inflammation/Immunology
    Demethylzeylasteral is a triterpene compound isolated from Tripterygium wilfordii Hook F, with anti-inflammatory, immunosuppressive and anti-tumor activities. Demethylzeylasteral can significantly alleviates atherosclerosis (AS). Demethylzeylasteral inhibits triple-negative breast cancer invasion by blocking the canonical and non-canonical TGF-β signaling pathways.
  • HY-116084
    Trimethylamine N-oxide

    NOD-like Receptor (NLR) Reactive Oxygen Species TGF-beta/Smad Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease
    Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.
  • HY-128859
    EMT inhibitor-2

    Cytochrome P450 Metabolic Disease
    EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively.
  • HY-B0673S
    Pirfenidone-d5

    AMR69-d5

    TGF-beta/Smad CCR Cancer Inflammation/Immunology
    Pirfenidone D5 (AMR69 D5) is a deuterium labeled Pirfenidone. Pirfenidone 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.
  • HY-12274
    ML347

    LDN 193719

    TGF-β Receptor Cancer
    ML347 (LDN193719) is a highly selective ALK1/ALK2 inhibitor. ML347 has IC50 values of 46 and 32 nM against ALK1 and ALK2, respectively, >300-fold selective over ALK3. ML347 block the phosphorylation of Smad1/5 by TGF-β1.
  • HY-138657
    NCGC00378430

    Phosphatase Cancer
    NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model.
  • HY-108915
    Trimethylamine N-oxide dihydrate

    NOD-like Receptor (NLR) Reactive Oxygen Species TGF-beta/Smad Endogenous Metabolite Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    Trimethylamine N-oxide dihydrate is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide dihydrate induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide dihydrate also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.
  • HY-B0252S
    Hydrochlorothiazid-d2

    HCTZ-d2

    TGF-beta/Smad Potassium Channel Metabolic Disease Cardiovascular Disease
    Hydrochlorothiazid-d2 (HCTZ-d2) is the deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic drug of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.
  • HY-B0252S1
    Hydrochlorothiazid-13C,d2

    HCTZ-13C,d2

    TGF-beta/Smad Potassium Channel Metabolic Disease Cardiovascular Disease
    Hydrochlorothiazid-13C,d2 is the 13C- and deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic drug of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.
  • HY-145532
    S-Allylmercaptocysteine

    Apoptosis NF-κB Keap1-Nrf2 Cancer Inflammation/Immunology
    S-allylmercaptocysteine, an organic sulfur compound extracted from garlic, has anti-inflammatory and anti-oxidative effects for various pulmonary diseases. S-allylmercaptocysteine achieves its anti-cancer effect through a variety of pathways such as inducing the apoptosis of cancer cells through the TGF-β signaling pathway, or reducing the NF-κB activity and up-regulating Nrf2 to achieve the effects of anti-inflammation and anti-oxidation.
  • HY-116084S
    Trimethylamine N-oxide-d9

    NOD-like Receptor (NLR) Reactive Oxygen Species TGF-beta/Smad Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease
    Trimethylamine N-oxide-d9 is the deuterium labeled Trimethylamine N-oxide. Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.
  • HY-135581
    Raloxifene 6-glucuronide

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-118528A
    TP0427736 hydrochloride

    TGF-β Receptor Endocrinology
    TP0427736 hydrochloride is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50=836 nM). TP0427736 hydrochloride also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. TP0427736 hydrochloride can be used for the research of androgenic alopecia (AGA).
  • HY-N1326
    Santamarine

    Santamarin; Balchanin

    Others Inflammation/Immunology
    Santamarine (Santamarin), a sesquiterpene lactone, increases HO-1 expression through Nrf2 translocation and suppresses NO, PGE2, TNF-α, and IL-1β production through inhibition of NF-κB translocation in LPS-induced macrophages. Santamarine shows anti-photoaging properties via inhibition of MAPK/AP-1 and stimulation of TGF-β/Smad signaling in UVA-irradiated human dermal fibroblasts (HDFs). Antioxidant activities.
  • HY-110246
    Quin C1

    Others Inflammation/Immunology
    Quin C1 is a highly specific and potent agonist for formyl peptide receptor 2 (FPR2/ALX). Quin-C1 significantly reduces the neutrophil and lymphocyte counts in BALF, diminishes expression of TNF-α, IL-1β, KC, and TGF-β1, and decreases collagen deposition in lung tissue. Quin C1 has the potential for the research of lung injury.
  • HY-124745
    KY-05009

    MAP4K Wnt Apoptosis Cancer
    KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.
  • HY-135582
    Raloxifene 4'-glucuronide

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-144437
    ALK5-IN-9

    TGF-β Receptor Cancer
    ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC50 values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease.
  • HY-N1584
    Halofuginone

    RU-19110

    DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel Cancer Infection Inflammation/Immunology Cardiovascular Disease
    Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
  • HY-100434
    PD-161570

    FGFR PDGFR EGFR Src TGF-β Receptor Cancer Cardiovascular Disease
    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.
  • HY-N1584A
    Halofuginone hydrobromide

    RU-19110 hydrobromide

    DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel Cancer Infection Inflammation/Immunology Cardiovascular Disease
    Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
  • HY-135581S
    Raloxifene 6-glucuronide-d4

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 6-glucuronide-d4 is the deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-130437
    p-nitro-Pifithrin-α

    MDM-2/p53 TGF-β Receptor Caspase Infection Metabolic Disease
    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.
  • HY-135581S1
    Raloxifene 6-glucuronide-d4 lithium

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-135582S1
    Raloxifene 4'-glucuronide-d4 lithium

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 4'-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-147946
    PDE1-IN-4

    Phosphodiesterase (PDE) Calcium Channel Inflammation/Immunology
    PDE1-IN-4 (compound 2g) is a potent and selective PDE1 (phosphodiesterase-1) inhibitor, with IC50 values of 10, 145, and 354 nM for PDE1C, PDE1A, and PDE1B, respectively. PDE1-IN-4 inhibits myofibroblast differentiation of human lung fibroblasts induced by TGF-β1. PDE1-IN-4 shows anti-fibrosis effects through the regulation of cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate). PDE1-IN-4 can be used for idiopathic pulmonary fibrosis (IPF) research.
  • HY-141645
    IMM-H007

    WS070117

    TGF-β Receptor AMPK NF-κB JNK AP-1 Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    IMM-H007 is a potent TGFβ1 (transforming growth factor β1) antagonist. IMM-H007 has protective effects in cardiovascular diseases via activation of AMPK (AMP-activated protein kinase). 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.