Transforming growth factor beta receptors

Pathways Recommended:	TGF-beta/Smad

By Targets:	TGF-beta/Smad (3) TGF-β Receptor (7) Apoptosis (3) Organoid (1) PI3K (3)
By Research Areas:	Cancer (9) Inflammation/Immunology (2) Metabolic Disease (1)

Targets Recommended: TGF-beta/Smad TGF-β Receptor FGFR VEGFR PDGFR Amyloid-β GHSR Beta-secretase 17β-HSD β-catenin 11β-HSD Beta-lactamase EGFR IGF-1R Dopamine β-hydroxylase Nuclear Hormone Receptor 4A/NR4A

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-12043

SB 525334

5+ Cited Publications

TGF-β Receptor Cancer

SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC₅₀ of 14.3 nM.

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.

SB 525334 5+ Cited Publications	TGF-β Receptor	Cancer
SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC₅₀ of 14.3 nM.

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-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-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-13012

RepSox Maximum Cited Publications 16 Publications Verification E-616452; SJN 2511	Organoid TGF-β Receptor	Metabolic Disease
RepSox (E-616452) is a potent and selective **transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC₅₀** value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes .

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-18758

IN-1130
IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC₅₀ of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC₅₀=36 nM) and p38α mitogen-activated protein kinase (IC₅₀=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis .

Cat. No.	Product Name

HY-L018

TGF-beta/Smad Compound Library	223 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 223 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.

TGF-beta/Smad Compound Library

223 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 223 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.

Cat. No.	Product Name	Target	Research Area

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 .

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 .

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