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Pathways Recommended: MAPK/ERK Pathway
Results for "

fibrosis pathway

" in MedChemExpress (MCE) Product Catalog:

67

Inhibitors & Agonists

2

Screening Libraries

8

Peptides

23

Natural
Products

7

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P10899

    TGF-beta/Smad PROTACs Endocrinology
    ETTAC-2 is a LRG1 PROTAC degrader. ETTAC-2 promotes ubiquitination and degradation of LRG1 (DC50 of 8.38 µM). ETTAC-2 inhibits the TGF-β-Smad3 signaling pathway and diminishes the secretion of fibrosis-associated proteins. ETTAC-2 attenuates the progression of renal fibrosis .
    ETTAC-2
  • HY-W005379

    TGF-beta/Smad Inflammation/Immunology
    DGM is an inhibitor of the TGF-β1/Smad signaling pathway with significant antifibrotic effects. DGM inhibits the epithelial-mesenchymal transition (EMT) process in alveolar epithelial cells and slows the progression of pulmonary fibrosis in vivo by reducing lung inflammation, improving lung function, and decreasing extracellular matrix (ECM) remodeling. DGM can be used in research on idiopathic pulmonary fibrosis (IPF) and EMT-related diseases .
    DGM
  • HY-N0546

    Nuezhenoside

    CaSR RIP kinase Mixed Lineage Kinase TGF-beta/Smad Cardiovascular Disease Neurological Disease Metabolic Disease Endocrinology
    Ligustroflavone is an orally active flavonoid compound. Ligustroflavone can be extracted from Ligustrum lucidum. Ligustroflavone antagonizes the calcium-sensing receptor (CaSR), inhibits the RIPK1/RIPK3/MLKL pathway, and downregulates TGF-β/Smad signaling. Ligustroflavone regulates calcium metabolism, protects bone tissue, reduces cerebral ischemic injury, and inhibits liver fibrosis. Ligustroflavone can be used in the study of diabetic osteoporosis, ischemic stroke, and liver fibrosis .
    Ligustroflavone
  • HY-111432

    Ras Others
    CCG-232601 (compound 8f) is a potent and orally active Rho/MRTF/SRF transcriptional pathway inhibitor. CCG-232601 inhibits the development of Bleomycin-induced dermal fibrosis in mice. CCG-232601 has the potential for the research of antifibrotic for systemic scleroderma .
    CCG-232601
  • HY-W018197

    Endogenous Metabolite p38 MAPK Reactive Oxygen Species Metabolic Disease Inflammation/Immunology Cancer
    2-Phenylacetamide is a estrogen-like compound that can be isolated from Lepidium apetalum seeds. 2-Phenylacetamide inhibits p38 MAPK signaling pathway, exhibits anti-inflammatory, antioxidant, anti-hypertensive, and anti-fibrosis effects. 2-Phenylacetamide is orally active .
    2-Phenylacetamide
  • HY-N13208

    MMP TGF-beta/Smad Others
    Stevia Powder is a natural sweetener with antioxidant activity. Stevia Powder can downregulate pro fibrotic pathways in cirrhotic rats, including reduced hepatic myofibroblasts and decreased expression of matrix metalloproteinases MMP2 and MMP13, upregulate anti fibrotic molecule Smad7, prevent serum necrosis and elevated bile stasis markers, thereby inhibiting the development of liver fibrosis .
    Stevia Powder
  • HY-N3674

    TGF-beta/Smad Inflammation/Immunology
    Dalbergioidin, a well-known anthocyanin, ameliorates doxorubicin-induced renal fibrosis by suppressing the TGF-β signal pathway. Dalbergioidin exhibits tyrosinase inhibitory activity with an IC50 of 20 mM .
    Dalbergioidin
  • HY-149403

    Anaplastic lymphoma kinase (ALK) Others
    J-1048 is an activin receptor-like kinase 5 (ALK5) inhibitor. J-1048 can inhibit TAA-induced liver fibrosis in mice by explicitly blocking the TGF-β/Smad signaling pathway .
    J-1048
  • HY-170839

    TRP Channel Inflammation/Immunology
    TRPV1-IN-3 (compound 14) is a TRPV1 inhibitor that can be used for the research of idiopathic pulmonary fibrosis. TRPV1-IN-3 affects the expression of fibrosis markers collagen I and α-SMA by inhibiting the TGF-β/Smads and MAPK pathways, thereby exerting antifibrotic activity in vitro (IC50=0.51 μM). TRPV1-IN-3 significantly inhibits collagen deposition in lung tissue, improves the alveolar structure, and also increases the survival rate of mice with pulmonary fibrosis induced by Bleomycin (HY-108345) .
    TRPV1-IN-3
  • HY-173480

    PARP Cancer
    TNKS-IN-3 (Compound 6) is a TNKS2 inhibitor (Ki: 8.5 nM). TNKS-IN-3 has good activity (IC50: 71 nM) and can effectively inhibit the WNT/β-catenin signaling pathway. TNKS-IN-3 can be used in the research of diseases such as cancer and fibrosis .
    TNKS-IN-3
  • HY-B0252
    Hydrochlorothiazide
    4 Publications Verification

    HCTZ

    TGF-beta/Smad Potassium Channel Cardiovascular Disease Metabolic Disease Cancer
    Hydrochlorothiazide (HCTZ), an orally active diuretic agent 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 .
    Hydrochlorothiazide
  • HY-121750

    Ras ROCK Cancer
    CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor . CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis .
    CCG-222740
  • HY-P6177

    Dipeptidyl Peptidase Inflammation/Immunology
    SGP8 (IAVPGEVA) is an octapeptide produced by hydrolysis of soybean 11S globulin, which has the effects of regulating lipid metabolism, inflammation and fibrosis. SGP8 (IAVPGEVA) exhibits inhibitory activity against DPP4 and inhibits the JNK-c-Jun signaling pathway, and has the ability to inhibit non-alcoholic steatohepatitis (NASH) .
    SGP8
  • HY-169963

    Phosphodiesterase (PDE) Others
    PDE1-IN-8 (Compound 3f) is the inhibitor for PDE1 with an IC50 of 11 nM. PDE1-IN-8 inhibits cAMP and cGMP signaling pathway, inhibits the differentiation and proliferation of cells into myofibroblast, and exhibits anti-fibrotic efficacy in Bleomycin (HY-17565)-induced rat pulmonary fibrosis model .
    PDE1-IN-8
  • HY-N0546R

    Nuezhenoside (Standard)

    Reference Standards CaSR RIP kinase Mixed Lineage Kinase TGF-beta/Smad Cardiovascular Disease Neurological Disease Metabolic Disease Endocrinology
    Ligustroflavone (Standard) is the analytical standard of Ligustroflavone (HY-N0546). This product is intended for research and analytical applications. Ligustroflavone is an orally active flavonoid compound. Ligustroflavone can be extracted from Ligustrum lucidum. Ligustroflavone antagonizes the calcium-sensing receptor (CaSR), inhibits the RIPK1/RIPK3/MLKL pathway, and downregulates TGF-β/Smad signaling. Ligustroflavone regulates calcium metabolism, protects bone tissue, reduces cerebral ischemic injury, and inhibits liver fibrosis. Ligustroflavone can be used in the study of diabetic osteoporosis, ischemic stroke, and liver fibrosis .
    Ligustroflavone (Standard)
  • HY-W753806

    UK 33274 hydrochloride

    Akt Cardiovascular Disease
    Doxazosin hydrochloride (UK 33274 hydrochloride) is a compound used to inhibit hypertension and prostate hyperplasia, with activity that inhibits postsynaptic α1-adrenoceptors on vascular smooth muscle. Doxazosin hydrochloride can cause vasodilation, thereby reducing peripheral vascular resistance. Doxazosin hydrochloride was found to inhibit the proliferation and migration of hepatic stellate cells in a mouse liver fibrosis model. Doxazosin hydrochloride regulates fibrosis, autophagy, and apoptosis of hepatic stellate cells by activating the PI3K/Akt/mTOR signaling pathway. Doxazosin hydrochloride also blocks autophagic flux and induces apoptosis of hepatic stellate cells .
    Doxazosin hydrochloride
  • HY-121246
    Fluorofenidone
    1 Publications Verification

    AKF-PD

    PI3K Akt Inflammation/Immunology
    Fluorofenidone (AKF-PD), an analogue of AMR69, shows equivalent antifibrotic activity, lower toxicity and longer half-life. Fluorofenidone (AKF-PD) attenuates the progression of renal interstitial fibrosis partly by suppressing NADPH oxidase and extracellular matrix (ECM) deposition via the PI3K/Akt signalling pathway .
    Fluorofenidone
  • HY-N0617
    Sanggenon C
    2 Publications Verification

    Phosphatase ERK NF-κB Apoptosis Cardiovascular Disease Inflammation/Immunology Cancer
    Sanggenon C, a flavonoid, exerts protective effects against cardiac hypertrophy and fibrosis via suppression of the calcineurin/NFAT2 pathway. Sanggenon C inhibits mitochondrial fission to induce apoptosis by blocking the ERK signaling pathway. Sanggenon C inhibits inducible nitric oxide synthase expression in RAW264.7 cells, and TNF-α-stimulated cell adhesion and VCAM-1 expression, by suppressing NF-κB activity. Sanggenon C possesses antioxidant, anti-inflammatory and antitumor activities .
    Sanggenon C
  • HY-128483

    TGF-beta/Smad PI3K NF-κB Akt Apoptosis Dopamine β-hydroxylase mTOR Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Fusaric acid is an orally active multi-pathway inhibitor with the activity of inducing oxidative stress and apoptosis. Fusaric acid can chelate divalent metal cations, damage mitochondrial membrane structure, and activate apoptosis-related proteases such as Caspase-3/7, -8, and -9. Fusaric acid also regulates Bax/Bcl-2 protein, inhibits fibrosis-related signaling pathways such as NF-κB, TGF-β1/SMADs, and PI3K/AKT/mTOR, and reduces collagen deposition. Fusaric acid is also a dopamine β-hydroxylase inhibitor, which reduces endogenous levels of norepinephrine and epinephrine in the brain, heart, spleen, and adrenal glands. Fusaric acid can play a role in myocardial fibrosis and improve cardiac hypertrophy in heart disease, and can also be used in the study of esophageal cancer and liver cancer .
    Fusaric acid
  • HY-N2329
    Piperlongumine
    5+ Cited Publications

    Piplartine

    ERK Reactive Oxygen Species Autophagy Apoptosis Bacterial Ferroptosis Infection Cardiovascular Disease Cancer
    Piperlongumine is a alkaloid , possesses ant-inflammatory, antibacterial, antiangiogenic, antioxidant, antitumor, and antidiabetic activities . Piperlongumine induces ROS, and induces apoptosis in cancer cell lines . Piperlongumine shows anti-cardiac fibrosis activity, suppresses myofibroblast transformation via suppression of the ERK1/2 signaling pathway. Piperlongumin could be used in the study of migrasome .
    Piperlongumine
  • HY-B0252S

    HCTZ-d2

    TGF-beta/Smad Potassium Channel Cardiovascular Disease Metabolic Disease
    Hydrochlorothiazid-d2 is the deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent 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 .
    Hydrochlorothiazid-d2
  • HY-116084
    Trimethylamine N-oxide
    5 Publications Verification

    Drug Metabolite NOD-like Receptor (NLR) Reactive Oxygen Species TGF-beta/Smad Endogenous Metabolite Cardiovascular Disease Inflammation/Immunology
    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 .
    Trimethylamine N-oxide
  • HY-B0252R
    Hydrochlorothiazide (Standard)
    4 Publications Verification

    HCTZ (Standard)

    TGF-beta/Smad Potassium Channel Cardiovascular Disease Metabolic Disease Cancer
    Hydrochlorothiazide (Standard) is the analytical standard of Hydrochlorothiazide. This product is intended for research and analytical applications. Hydrochlorothiazide (HCTZ), an orally active diuretic agent 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 .
    Hydrochlorothiazide (Standard)
  • HY-108915
    Trimethylamine N-oxide dihydrate
    5 Publications Verification

    NOD-like Receptor (NLR) Reactive Oxygen Species TGF-beta/Smad Endogenous Metabolite Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    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 .
    Trimethylamine N-oxide dihydrate
  • HY-B0252S2

    HCTZ-13C6

    TGF-beta/Smad Potassium Channel Metabolic Disease
    Hydrochlorothiazide- 13C6 is the 13C labeled Hydrochlorothiazide . Hydrochlorothiazide (HCTZ), an orally active diuretic agent 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 .
    Hydrochlorothiazide-13C6
  • HY-128439

    DYRK Cancer
    BT173 is a potent homeodomain interacting protein kinase 2 (HIPK2) inhibitor. BT173 binds to HIPK2 does not inhibit HIPK2 kinase activity but rather, interfered allosterically with the ability of HIPK2 to associate with Smad3. BT173 attenuates renal fibrosis through suppression of the TGF-β1/Smad3 pathway .
    BT173
  • HY-128483R

    TGF-beta/Smad PI3K NF-κB Akt Apoptosis Dopamine β-hydroxylase mTOR Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Fusaric acid (Standard) is the analytical standard of Fusaric acid (HY-128483). This product is intended for research and analytical applications. Fusaric acid is an orally active multi-pathway inhibitor with the activity of inducing oxidative stress and apoptosis. Fusaric acid can chelate divalent metal cations, damage mitochondrial membrane structure, and activate apoptosis-related proteases such as Caspase-3/7, -8, and -9. Fusaric acid also regulates Bax/Bcl-2 protein, inhibits fibrosis-related signaling pathways such as NF-κB, TGF-β1/SMADs, and PI3K/AKT/mTOR, and reduces collagen deposition. Fusaric acid is also a dopamine β-hydroxylase inhibitor, which reduces endogenous levels of norepinephrine and epinephrine in the brain, heart, spleen, and adrenal glands. Fusaric acid can play a role in myocardial fibrosis and improve cardiac hypertrophy in heart disease, and can also be used in the study of esophageal cancer and liver cancer .
    Fusaric acid (Standard)
  • HY-170540

    NADPH Oxidase TGF-beta/Smad Reactive Oxygen Species Inflammation/Immunology
    NOX4-IN-1 (Compound 14m) is the inhibitor for NADPH oxidase 4 (NOX4), and blocks the generation of ROS. NOX4-IN-1 inhibits TGF-β1/Smad signaling pathway, decreases the expression of fibrosis-related proteins. NOX4-IN-1 inhibits the cell migration of NRK-49F .
    NOX4-IN-1
  • HY-142698

    Guanylate Cyclase Cardiovascular Disease
    SGC agonist 2 is a potent agonist of soluble guanylate cyclase (SGC). Soluble guanylate cyclase is a key signal transduction enzyme in the NO-sGC-cGMP signaling pathway. SGC agonist 2 has the potential for the research of cardiovascular disease (heart failure, pulmonary hypertension, angina, myocardial infarction) and fibrotic diseases (renal fibrosis, systemic sclerosis) (extracted from patent WO2021219088A1, compound 031) .
    SGC agonist 2
  • HY-121246S

    AKF-PD-d3

    Isotope-Labeled Compounds Akt PI3K Inflammation/Immunology
    Fluorofenidone-d3 is deuterium labeled Fluorofenidone. Fluorofenidone (AKF-PD), an analogue of AMR69, shows equivalent antifibrotic activity, lower toxicity and longer half-life. Fluorofenidone (AKF-PD) attenuates the progression of renal interstitial fibrosis partly by suppressing NADPH oxidase and extracellular matrix (ECM) deposition via the PI3K/Akt signalling pathway .
    Fluorofenidone-d3
  • HY-W018197R

    Endogenous Metabolite p38 MAPK Reactive Oxygen Species Metabolic Disease Inflammation/Immunology Cancer
    2-Phenylacetamide (Standard) is the analytical standard of 2-Phenylacetamide. This product is intended for research and analytical applications. 2-Phenylacetamide is a estrogen-like compound that can be isolated from Lepidium apetalum seeds. 2-Phenylacetamide inhibits p38 MAPK signaling pathway, exhibits anti-inflammatory, antioxidant, anti-hypertensive, and anti-fibrosis effects. 2-Phenylacetamide is orally active .
    2-Phenylacetamide (Standard)
  • HY-170765

    Phosphodiesterase (PDE) Inflammation/Immunology
    ATX-IN-1 (compound 35) is an inhibitor of ATX (IC50=0.7 nM) with anti-inflammatory activity. ATX-IN-1 can inhibit TGF-β/Smad pathway and reduce collagen deposition to alleviate Bleomycin (HY-108345)-induced fibrosis in mice. ATX-IN-1 has good oral bioavailability (F=69.5%) and particle stability .
    ATX-IN-1
  • HY-B0252S1

    HCTZ-13C,d2

    Isotope-Labeled Compounds TGF-beta/Smad Potassium Channel Cardiovascular Disease Metabolic Disease
    Hydrochlorothiazid- 13C,d2 is the 13C- and deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent 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 .
    Hydrochlorothiazid-13C,d2
  • HY-N6985
    Baccatin III
    1 Publications Verification

    Others Cancer
    Baccatin III is an orally available, selective inhibitor of the TGF-β1 signaling pathway and myeloid-derived suppressor cell (MDSC) activation. Baccatin III targets the AKT/STAT6 and Smad2/3 pathways, blocking TGF-β1-induced fibroblast differentiation and MDSC-mediated immunosuppression. Baccatin III exerts anti-inflammatory and anti-fibrotic effects by inhibiting macrophage activation and extracellular matrix deposition, and shows potential in the treatment of pulmonary fibrosis and cancer in terms of regulating the tumor immune microenvironment[1][2].
    Baccatin III
  • HY-N0202
    Atractylenolide II
    3 Publications Verification

    Asterolide

    ERK Apoptosis p38 MAPK Akt Src STAT Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cell cycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
    Atractylenolide II
  • HY-112671

    RTA dh404

    Keap1-Nrf2 NF-κB Apoptosis Cardiovascular Disease Inflammation/Immunology
    CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB . CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats .
    CDDO-dhTFEA
  • HY-170813

    CDK TGF-beta/Smad Infection
    P162-0948 is a selective CDK8 inhibitor with an IC50 value of 50.4 nM. P162-0948 reduces cell migration and protein expression of EMT-related proteins in A549 human alveolar epithelial cell lines. P162-0948 reduces phosphorylation of Smad, which suggests disruption of the TGF-β/Smad signaling pathway. P162-0948 is promising for research of pulmonary fibrosis .
    P162-0948
  • HY-P10869

    Natriuretic Peptide Receptor (NPR) Inflammation/Immunology Cancer
    dCNP binds to NPR-B/C receptor, activates cGMP signaling pathway, and regulates vascular function. dCNP exhibits anti-hypoxia property through downregulation of hypoxia-related genes expressions like HIF1α and HIF2α. dCNP inhibits the induction of tumor stroma and exhibits anti-fibrosis activity. dCNP upregulates CTLs, NK cells, and conventional type 1 dendritic cells in tumors, and activates immune responses .
    dCNP
  • HY-116084S
    Trimethylamine N-oxide-d9
    1 Publications Verification

    NOD-like Receptor (NLR) Reactive Oxygen Species TGF-beta/Smad Endogenous Metabolite Cardiovascular Disease Inflammation/Immunology
    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 .
    Trimethylamine N-oxide-d9
  • HY-116084S1

    Isotope-Labeled Compounds NOD-like Receptor (NLR) Reactive Oxygen Species TGF-beta/Smad Endogenous Metabolite Cardiovascular Disease Inflammation/Immunology
    Trimethylamine-N-oxide- 13C3 is the 13C-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 .
    Trimethylamine-N-oxide-13C3
  • HY-N0512
    Loganin
    4 Publications Verification

    Loganoside

    Reactive Oxygen Species TNF Receptor Interleukin Related Neurological Disease Inflammation/Immunology Cancer
    Loganin is a type of iridoid glycoside compound that possesses anti-inflammatory, antioxidant, and antitumor properties, and offers protective effects against acute lung injury and pulmonary fibrosis. Loganin exerts its protective effects against LPS (HY-D1056)-mediated inflammation and oxidative stress by upregulating the Nrf2/HO-1 signaling pathway, and it reduces neuroinflammation caused by spinal cord injury (SCI) .
    Loganin
  • HY-N2013
    Aristolactam I
    1 Publications Verification

    Aristololactam; Aristolactam

    Drug Metabolite Aquaporin Cadherin TGF-beta/Smad Endocrinology Cancer
    Aristolactam I is an AQP1 inhibitor and Aristolochic acid I metabolite. Aristolactam I can be isolated from Aristolochia plants. Aristolactam I downregulates Twist1 expression, increases E-cadherin expression, and activates the TGF-β/Smad signaling pathway. Aristolactam I has anticancer activity against breast cancer. Aristolactam I is nephrotoxic. Aristolactam I is mainly used in the study of breast cancer and kidney diseases such as renal interstitial fibrosis .
    Aristolactam I
  • HY-W008947
    SEW​2871
    5+ Cited Publications

    LPL Receptor ERK Akt Neurological Disease Metabolic Disease Inflammation/Immunology
    SEW2871 is an orally active, potent, highly selective S1P1 (sphingosine-1-phosphate type 1 receptor) agonist, with an EC50 of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood. SEW2871 can be used for the research of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses .
    SEW​2871
  • HY-B0252S3

    HCTZ-15N2,13C,d2

    Potassium Channel TGF-beta/Smad Isotope-Labeled Compounds Cardiovascular Disease Metabolic Disease Cancer
    Hydrochlorothiazide- 15N2, 13C,d2 is 15N and deuterated labeled Hydrochlorothiazide (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent 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 .
    Hydrochlorothiazide-15N2,13C,d2
  • HY-162147

    mTOR Autophagy Inflammation/Immunology
    Nur77 modulator 3 (9e) can bind to Nur77 and inhibit TGF-β1-induced α-SMA and COLA1 expression in a Nur77-dependent manner. Nur77 modulator 3 induces Nur77 expression and enhances autophagic flux by inhibiting the mTORC1 signaling pathway in vitro and in vivo. Nur77 modulator 3 blocks the progression of hepatic fibrosis .
    Nur77 modulator 3
  • HY-170227

    Phosphodiesterase (PDE) TGF-β Receptor Inflammation/Immunology
    Autotaxin-IN-7 (45), a pyridine-2-carboxylic derivative, demonstrates subnanomolar ATX inhibition (IC50 = 0.086 nM), with a favorable heart safety profile (hERG > 30 μM) and minimal fibroblast toxicity. Autotaxin-IN-7 (45) suppresses the TGF-β/Smad signaling pathway, downregulating α-smooth muscle actin (α-SMA) and extracellular matrix components (ECM). Autotaxin-IN-7 (45) is used in the research for pulmonary fibrosis .
    Autotaxin-IN-7
  • HY-N0247

    Hedgehog Smo STAT Interleukin Related TNF Receptor Inflammation/Immunology Cancer
    Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the 5-HT2C receptor with an EC50 of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer activities thus can be studies in research for cancers such as Medulloblastoma (MB) .
    Saikosaponin B1
  • HY-D0961

    Fluorescent Dye Wnt β-catenin Neurological Disease Inflammation/Immunology Cancer
    Gallocyanine chloride is a synthetic blue dyestuff that can be used as a potential agent for the research of Alzheimer's disease and related neurodegenerative tauopathies. Gallocyanine chloride inhibits DKK1/LRP6 interaction (IC50=6.38 μM), activates Wnt signaling pathway, and causes β-catenin accumulation. Gallocyanine chloride exhibits anti-metastasis, anti-inflammatory and anti-fibrosis activities. Gallocyanine chloride can be used as a fluorescent probe for detection of superoxide anion radicals .
    Gallocyanine chloride
  • HY-151483

    Wnt Histone Demethylase Cardiovascular Disease
    TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease .
    TK-129
  • HY-108464A

    Sodium Channel TRP Channel Metabolic Disease Inflammation/Immunology
    Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM . Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca 2+ transport with an IC50 of 140 nM in a Ca 2+ uptake assay . Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway . Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease .
    Phenamil methanesulfonate

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