Search Result

Pathways Recommended:	TGF-beta/Smad

Results for "

TGF beta inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	TGF-beta/Smad (35) TGF-β Receptor (46) AMPK (1) Anaplastic lymphoma kinase (ALK) (4) Antibiotic (1) AP-1 (1) Apoptosis (15) Autophagy (3) Bacterial (2) Biochemical Assay Reagents (1) Calcium Channel (4) Caspase (1) Cytochrome P450 (1) DNA/RNA Synthesis (3) DYRK (1) Endogenous Metabolite (2) ERK (1) Estrogen Receptor/ERR (5) FLT3 (1) FXR (1) GPR68 (1) HDAC (2) HSP (1) Integrin (3) Interleukin Related (1) Isotope-Labeled Compounds (3) JNK (1) MAP3K (1) MAP4K (2) MDM-2/p53 (1) Microtubule/Tubulin (1) MMP (1) mTOR (1) Myosin (1) NF-κB (3) Organoid (4) p38 MAPK (1) Parasite (3) PD-1/PD-L1 (2) PDGFR (1) Phosphatase (1) Phosphodiesterase (PDE) (2) PI3K (3) Potassium Channel (6) Protease Activated Receptor (PAR) (2) Reactive Oxygen Species (1) Sodium Channel (3) STAT (4) TAM Receptor (2) Toll-like Receptor (TLR) (2) VD/VDR (1) Wnt (1)
By Research Areas:	Cancer (70) Cardiovascular Disease (15) Endocrinology (6) Infection (8) Inflammation/Immunology (35) Metabolic Disease (11) Neurological Disease (3)

By Targets:

TGF-beta/Smad (35)

TGF-β Receptor (46)

AMPK (1)

Anaplastic lymphoma kinase (ALK) (4)

Antibiotic (1)

AP-1 (1)

Apoptosis (15)

Autophagy (3)

Bacterial (2)

Biochemical Assay Reagents (1)

Calcium Channel (4)

Caspase (1)

Cytochrome P450 (1)

DNA/RNA Synthesis (3)

DYRK (1)

Endogenous Metabolite (2)

ERK (1)

Estrogen Receptor/ERR (5)

FLT3 (1)

FXR (1)

GPR68 (1)

HDAC (2)

HSP (1)

Integrin (3)

Interleukin Related (1)

Isotope-Labeled Compounds (3)

JNK (1)

MAP3K (1)

MAP4K (2)

MDM-2/p53 (1)

Microtubule/Tubulin (1)

MMP (1)

mTOR (1)

Myosin (1)

NF-κB (3)

Organoid (4)

p38 MAPK (1)

Parasite (3)

PD-1/PD-L1 (2)

PDGFR (1)

Phosphatase (1)

Phosphodiesterase (PDE) (2)

PI3K (3)

Potassium Channel (6)

Protease Activated Receptor (PAR) (2)

Reactive Oxygen Species (1)

Sodium Channel (3)

STAT (4)

TAM Receptor (2)

Toll-like Receptor (TLR) (2)

VD/VDR (1)

Wnt (1)

By Research Areas:

Cancer (70)

Cardiovascular Disease (15)

Endocrinology (6)

Infection (8)

Inflammation/Immunology (35)

Metabolic Disease (11)

Neurological Disease (3)

117

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Inhibitory Antibodies

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Targets Recommended: TGF-β Receptor TGF-beta/Smad Amyloid-β Beta-secretase 17β-HSD β-catenin 11β-HSD Beta-lactamase Dopamine β-hydroxylase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-128437

TGFβ-IN-5

TGF-β Receptor Inflammation/Immunology

TGFβ-IN-5(Compd 12) is a TGFβ inhibitor useful for the study of fibroproliferative diseases associated with TGF-β signaling .

TGFβ-IN-5	TGF-β Receptor	Inflammation/Immunology
TGFβ-IN-5(Compd 12) is a TGFβ inhibitor useful for the study of fibroproliferative diseases associated with TGF-β signaling .

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-151427

TGFβ1-IN-1	TGF-β Receptor	Inflammation/Immunology
TGFβ1-IN-1 (compound 42) is a potent, orally active *TGF-β1* inhibitor. TGFβ1-IN-1 inhibits the upregulation of TGF-β1-induced fibrosis markers (α-SMA and fibronectin) and can be used in liver fibrosis disease studies .

HY-P5542

Vicatertide

SB-01
TGF-β Receptor Inflammation/Immunology

Vicatertide is a TGF beta-1 inhibitor .

Vicatertide SB-01	TGF-β Receptor	Inflammation/Immunology
Vicatertide is a **TGF beta-1** inhibitor .

HY-161398

TGFβRI-IN-7	TGF-β Receptor TGF-beta/Smad	Cancer
TGFβRI-IN-7 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) (IC₅₀ = 4.1 μM). TGFβRI-IN-7 inhibits TGFβ signaling by promoting the proteolytic degradation of TGFβ RII. TGFβRI-IN-7 can block endothelial-to-mesenchymal transition and cell migration. TGFβRI-IN-7 can be used in cancer research .

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-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-142118A

Trabedersen sodium AP 12009 sodium	TGF-beta/Smad	Cancer
Trabedersen sodium is an antisense oligodeoxynucleotide that specifically inhibits *TGF-β2* (TGF-beta/Smad). Trabedersen sodium can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon .

HY-142118

Trabedersen AP 12009	TGF-beta/Smad	Cancer
Trabedersen (AP 12009) is an antisense oligodeoxynucleotide that specifically inhibits *TGF-β2* (TGF-beta/Smad). Trabedersen can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon .

HY-13226

Galunisertib 35+ Cited Publications 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-118810

BIO-013077-01

TGF-β Receptor Cancer

BIO-013077-01 is a pyrazole TGF-β inhibitor .

BIO-013077-01	TGF-β Receptor	Cancer
BIO-013077-01 is a pyrazole *TGF-β* inhibitor .

HY-P990107

Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11)	Others	Inflammation/Immunology
Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11) is an anti-mouse/human/rat/monkey/hamster/canine/bovine IgG antibody inhibitor of TGF-β .

HY-163536

TGF-β1/Smad3-IN-1	TGF-beta/Smad	Inflammation/Immunology
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 .

HY-N0439

Asiaticoside 5+ Cited Publications	TGF-beta/Smad Reactive Oxygen Species Apoptosis Endogenous Metabolite	Cardiovascular Disease Neurological Disease Inflammation/Immunology 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-101275

EMT inhibitor-1

2 Publications Verification

EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.
HY-12704

ITD-1

4 Publications Verification

TGF-β Receptor Cardiovascular Disease

ITD-1 is the first selective TGFβ receptor inhibitor with an IC₅₀ of 460 nM.
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.

EMT inhibitor-1 2 Publications Verification
EMT inhibitor-1 is an inhibitor of of Hippo, *TGF-β, and Wnt* signaling pathways with antitumor activities.

ITD-1 4 Publications Verification	TGF-β Receptor	Cardiovascular Disease
ITD-1 is the first selective TGFβ receptor inhibitor with an IC₅₀ of 460 nM.

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-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-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-155699

J27644

HDAC Inflammation/Immunology

J27644 is a potent HDAC inhibitor. J27644 mitigates TGF-β-induced pulmonary fibrosis .

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.

J27644	HDAC	Inflammation/Immunology
J27644 is a potent HDAC inhibitor. J27644 mitigates TGF-β-induced pulmonary fibrosis .

HY-137561

Bexotegrast PLN-74809	Integrin	Inflammation/Immunology
Bexotegrast (PLN-74809) is an orally active, potent dual αvβ6/αvβ1 integrin inhibitor with K_d of 5.7 nM and 3.4 nM, respectively. Bexotegrast inhibits αvβ6- and αvβ1-induced TGF-β activation with IC₅₀ values of 29.8 nM and 19.2 nM, respectively. Bexotegrast has antifibrogenic effects and block multiple avenues of TGF-β activation in the fibrotic lung .

HY-12075

LY2109761 40+ Cited Publications	TGF-β Receptor Autophagy	Cancer
LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with K_is of 38 nM and 300 nM, respectively.

HY-W107024

BMS-986260	TGF-β Receptor	Inflammation/Immunology Cancer
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-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-W105318

Pentabromophenol PBP	TGF-beta/Smad Apoptosis	Cancer
Pentabromophenol (PBP) is a brominated flame retardant (BFR) widely used in various consumer products to reduce the flammability of materials used in different utility items. Pentabromophenol can accelerate the degradation of transforming growth factor-β (TGF-β) receptors by promoting clathrin-mediated endocytosis, thereby inhibiting the *TGF-β* signaling pathway. Additionally, Pentabromophenol can also induce apoptosis in peripheral blood mononuclear cells (PBMCs) .

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-P0299A

LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA) 5+ Cited Publications	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-P0299

LSKL, Inhibitor of Thrombospondin (TSP-1) 5+ Cited Publications	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-N10577

Chlorfortunone A	TGF-beta/Smad	Cancer
Chlorfortunone A is a novel sesquiterpenoid dimers, can be isolated from the roots of Chloranthus fortunei. Chlorfortunone A inhibits transforming growth factor (TGF)-β activity .

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-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-161400

TGFβRII-IN-2	TGF-β Receptor	Cancer
TGFβRII-IN-2 (Compound 3n) is an inhibitor for transforming growth factor-β type II receptor (TGFβRII) with IC₅₀ of 2.4 μM, which blocks endothelial-to-mesenchymal transition and cell migration in different cancer cell lines without perturbing the microtubule network .

HY-78349

A 77-01 1 Publications Verification	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-10431

SB-431542 Maximum Cited Publications 164 Publications Verification	Organoid TGF-β Receptor Apoptosis	Cancer
SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC₅₀ values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways .

HY-100608

BMS453 1 Publications Verification BMS-189453
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-N2092

Atractylodinol	Bacterial	Infection Cancer
Atractylodinol, an antimicrobial, is a PRRSV (porcine reproductive and respiratory syndrome virus) inhibitor. Atractylodinol inhibits TGF-β receptor I recycling by binding to vimentin (K_D of 454 nM) and inducing the formation of filamentous aggregates .

HY-10326

GW788388 10+ Cited Publications	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-151279

ALK5-IN-30

Anaplastic lymphoma kinase (ALK) Cancer

ALK5-IN-30 (EX-07) is a potent ALK inhibitor, inhibits ALK5 and TGFβ-R1 with both IC₅₀s <10 nM .

ALK5-IN-30	Anaplastic lymphoma kinase (ALK)	Cancer
ALK5-IN-30 (EX-07) is a potent ALK inhibitor, inhibits ALK5 and TGFβ-R1 with both IC₅₀s <10 nM .

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-142949

ALK5-IN-7	TGF-β Receptor	Inflammation/Immunology Cancer
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	TGF-β Receptor	Inflammation/Immunology Cancer
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-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-150169

THRX-144644	TGF-β Receptor	Cancer
THRX-144644 is a Lung-restricted ALK5 inhibitor with an IC₅₀ value of 0.14 nM. THRX-144644 avoids systemic toxicities associated with TGFβ pathway inhibition .

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-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 TFA is also a PI3K inhibitor and an apoptosis inducer .

HY-P0118B

Disitertide diammonium 10+ Cited Publications P144 diammonium	TGF-beta/Smad PI3K Apoptosis	Cancer
Disitertide (P144) diammonium is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide diammonium is also a PI3K inhibitor and an apoptosis inducer .

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-146205

ATX inhibitor 18	Phosphodiesterase (PDE)	Cardiovascular Disease
ATX inhibitor 18 is a potent ATX inhibitor with an IC₅₀ value of 24.2 nM. ATX inhibitor 18 shows antiproliferative activity and anti-fibrosis activity. ATX inhibitor 18 suppresses collagen deposition in TGF-β-mediated cardiac fibrosis .

HY-P99708

Livmoniplimab ABBV-151; ARGX-115	TGF-beta/Smad	Cancer
Livmoniplimab (ABBV-151; ARGX-115) is a potent, humanized monoclonal antibody against the LRRC32 (GARP)/TGFβ1 complex. Livmoniplimab blocks LRRC32-mediated latent TGFβ1 activation and release. Livmoniplimab has potential in cancer research as a single anticancer agent or in combination with an anti-PD-1 mAb to inhibit locally advanced or metastatic solid tumors (NCT03821935) .

HY-13013

SIS3 70+ Cited Publications	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 .

Cat. No.	Product Name

HY-L018

TGF-beta/Smad Compound Library

226 compounds

The transforming growth factor beta (TGF-β) signaling pathway is involved in many cellular processes in both the adult organism and the developing embryo including cell growth, cell differentiation, apoptosis, cellular homeostasis and other cellular functions. The TGF-β superfamily comprises TGF-βs, bone morphogenetic proteins (BMPs), activins and related proteins. Signaling begins with the binding of a TGF beta superfamily ligand to a TGF beta type II receptor. The type II receptor is a serine/threonine receptor kinase, which catalyzes the phosphorylation of the Type I receptor. The type I receptor then phosphorylates receptor-regulated SMADs (R-SMADs) which can now bind the coSMAD (e.g. SMAD4). R-SMAD/coSMAD complexes accumulate in the nucleus where they act as transcription factors and participate in the regulation of target gene expression. Deregulation of TGF-β signaling contributes to developmental defects and human diseases, including cancers, some bone diseases, chronic kidney disease, etc.

MCE designs a unique collection of 226 TGF-beta/Smad signaling pathway compounds. TGF-beta/Smad Compound Library acts as a useful tool for TGF-beta/Smad-related drug screening and disease research.

HY-L088

2003 compounds

Angiogenesis is the physiological process through which new blood vessels are formed from pre-existing vessels. It occurs in various physiological processes e.g. embryonic development, menstrual cycle, exercise and wound healing etc. Angiogenesis is regulated by both endogenous activators and inhibitors. Some key activators of angiogenesis include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), angiogenin, TGF-β, etc. whereas angiogenesis inhibitors are angiostatin, endostatin, interferon, platelet factor 4, etc. The loss of balance between these opposing signals leads to life threatening diseases like cancer, cardiovascular and ischemic diseases etc. which are thus controlled by exogenous angiogenesis activators (for cardiovascular/ischemic disorders) and inhibitors (for cancer).

MCE offers a unique collection of 2003 compounds with validated angiogenesis targets modulating properties. MCE angiogenesis-related compound library is an effective tool for angiogenesis research and discovery of angiogenesis-related drugs.

Cat. No.	Product Name	Target	Research Area

HY-P0299A

LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA) 5+ Cited Publications	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-P0299

LSKL, Inhibitor of Thrombospondin (TSP-1) 5+ Cited Publications	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-P5542

Vicatertide

SB-01
TGF-β Receptor Inflammation/Immunology

Vicatertide is a TGF beta-1 inhibitor .

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-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 TFA is also a PI3K inhibitor and an apoptosis inducer .

HY-P0118B

Disitertide diammonium Maximum Cited Publications 11 Publications Verification P144 diammonium	TGF-beta/Smad PI3K Apoptosis	Cancer
Disitertide (P144) diammonium is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide diammonium is also a PI3K inhibitor and an apoptosis inducer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0439

Asiaticoside 5+ Cited Publications	Cardiovascular Disease Triterpenes Structural Classification Neurological Disease Classification of Application Fields Source classification Tagetes lucida Cav. Plants Endogenous metabolite Terpenoids Umbelliferae Disease Research Fields Cancer	TGF-beta/Smad Reactive Oxygen Species Apoptosis Endogenous Metabolite
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-N6896

Isoviolanthin	Flavonoids other families Classification of Application Fields Flavones Source classification Phenols Polyphenols Plants Disease Research Fields Cancer	TGF-beta/Smad
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-N10577

Chlorfortunone A	Structural Classification Terpenoids Sesquiterpenes Chloranthaceae Plants Chloranthus fortunei (A. Gray) Solms-Laub	TGF-beta/Smad
Chlorfortunone A is a novel sesquiterpenoid dimers, can be isolated from the roots of Chloranthus fortunei. Chlorfortunone A inhibits transforming growth factor (TGF)-β activity .

HY-N10438

Ganodermaones B	Other Terpenoids Structural Classification Microorganisms Classification of Application Fields Terpenoids Source classification Inflammation/Immunology Disease Research Fields	Integrin
Ganodermaones B (Compound 2) is a renal fibrosis inhibitor. Ganodermaones B inhibits TGF-β1-induced collagen I and fibronectin expression .

HY-N2092

Atractylodinol	Structural Classification Natural Products Source classification Plants Compositae Erythrina sigmoidea Hua	Bacterial
Atractylodinol, an antimicrobial, is a PRRSV (porcine reproductive and respiratory syndrome virus) inhibitor. Atractylodinol inhibits TGF-β receptor I recycling by binding to vimentin (K_D of 454 nM) and inducing the formation of filamentous aggregates .

HY-113604

Pentabromopseudilin	Structural Classification Natural Products Source classification Marine natural products Marine microorganism	TGF-β Receptor
Pentabromopseudilin (PBrP) is a marine antibiotic isolated from the marine bacteria Pseudomonas bromoutilis and Alteromonas luteoviolaceus. PBrP exhibits antimicrobial, anti-tumour and phytotoxic activities. PBrP is a reversible and allosteric inhibitor of myosin Va (MyoVa). PBrP also is a potent inhibitor of *transforming growth factor-β (TGF-β)* activity. PBrP can be used for the research of fibrotic diseases and cancer .

HY-N6679A

10,11-Dehydrocurvularin	Infection Structural Classification Microorganisms Macrolide Antibiotics Classification of Application Fields Antibiotics Source classification Phenols Polyphenols Disease Research Anticancer Disease Research Fields	HSP TGF-beta/Smad
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-N0158

Oxymatrine Maximum Cited Publications 12 Publications Verification	Infection Alkaloids Piperidine Alkaloids Structural Classification Classification of Application Fields Leguminosae Source classification Plants Sophora flavescens Aiton Inflammation/Immunology Disease Research Fields	TGF-beta/Smad Apoptosis
Oxymatrine, an alkaloid from Sophora flavescens Alt. 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-N11768

4-Methoxylonchocarpin	Structural Classification Monophenols Source classification Phenols Plants Moraceae Dorstenia mannii Hook.f.	NF-κB Interleukin Related Toll-like Receptor (TLR)
4-Methoxylonchocarpin is an orally active anti-inflammatory agent. 4-methoxylonchocarpin inhibits the binding of LPS to Toll-like Receptor (TLR) TLR4 to inhibit NF-κB activation and TNF Receptor and IL-6 expression. 4-Methoxylonchocarpin also inhibits the phosphorylation of TGF-beta activated kinase 1 and TNBS-induced expression of IL-1β, IL-17A, and TNF. 4-methoxylonchocarpin can improve 2,4, 6-trinitrobenzene sulfonic acid (TNBS)-induced colitis mouse model .

HY-N0587

Demethylzeylasteral 2 Publications Verification	Triterpenes Classification of Application Fields Terpenoids Source classification Celastraceae Plants Tripterygium wilfordii Hook. f. Inflammation/Immunology Disease Research Fields	Apoptosis
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-W012977

3,3-Dimethyl-1-butanol DMB; Neohexanol	Structural Classification Natural Products Classification of Application Fields Source classification Metabolic Disease Endogenous metabolite Inflammation/Immunology Disease Research Fields	TGF-beta/Smad NF-κB Endogenous Metabolite
3,3-Dimethyl-1-butanol (DMB) is an orally active inhibitor of trimethylamine (TMA) and trimethylamine N-oxide (TMAO). 3,3-Dimethyl-1-butanol inhibits the signaling pathway of p65 NF-κB and *TGF-β1/Smad3*. 3,3-Dimethyl-1-butanol has potential applications in cardiovascular disease (CVD) .

HY-N1584

Halofuginone 5+ Cited Publications RU-19110	Infection Cardiovascular Disease Alkaloids Piperidine Alkaloids Structural Classification Classification of Application Fields Dichroa febrifuga Lour Source classification Saxifragaceae Plants Inflammation/Immunology Disease Research Fields	DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel
Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i 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-N1584A

Halofuginone hydrobromide 5+ Cited Publications RU-19110 hydrobromide	Infection Cardiovascular Disease Alkaloids Piperidine Alkaloids Structural Classification Classification of Application Fields Dichroa febrifuga Lour Source classification Saxifragaceae Plants Inflammation/Immunology Disease Research Fields	DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel
Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i 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-N1346

Robinin 1 Publications Verification	Structural Classification Flavonoids Classification of Application Fields Flavones Leguminosae Plants Vigna unguiculata Inflammation/Immunology Disease Research Fields	Toll-like Receptor (TLR) Apoptosis
Robinin is a flavonoid that can be extracted from the leaves of purple cowpea, inhibiting TGF-β, TLR4/NF-κB and TLR2-PI3k-AKT signaling pathways. Robinin exerts anti-inflammatory and anti-tumor effects. The combination of Robinin and Methotrexate (HY-14519) reduces inflammation in experimental arthritis, Robinin can decrease the Doxorubicin (HY-15142A) induced cardiac toxicity effect .

Cat. No.	Product Name	Chemical Structure

HY-B0252S

Hydrochlorothiazid-d2

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[1][2][3].

HY-B0252S2

Hydrochlorothiazide-13C6

Hydrochlorothiazide- ¹³C₆ is the ¹³C labeled Hydrochlorothiazide[1]. 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[2][3][4].

HY-B0252S1

Hydrochlorothiazid-13C,d2

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[1][2][3].

HY-B0252S3

Hydrochlorothiazide-15N2,13C,d2

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 .

HY-135581S1

Raloxifene 6-glucuronide-d4 lithium

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[1][2][3].

HY-135582S1

Raloxifene 4'-glucuronide-d4 lithium

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. [1][2]. 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[3].

HY-135582S

Raloxifene 4'-glucuronide-d4

Raloxifene 4'-glucuronide-d₄ is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). 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 .

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