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Pathways Recommended:	TGF-beta/Smad

Results for "

transforming growth factor-beta type I receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	TGF-beta/Smad (1) TGF-β Receptor (8) Anaplastic lymphoma kinase (ALK) (1) Isotope-Labeled Compounds (1) Organoid (2) Reference Standards (1)
By Research Areas:	Cancer (4) Inflammation/Immunology (3) Metabolic Disease (4)

Inhibitors & Agonists

Screening Libraries

Isotope-Labeled Compounds

Targets Recommended: TGF-β Receptor TGF-beta/Smad C-type Lectin-like Receptors (CTLRs) FGFR PCSK9 GHR VEGFR PDGFR EGFR IGF-1R GHSR Scavenger Receptor Class B type I (SR-BI） Nuclear Hormone Receptor 4A/NR4A

Cat. No.	상품명	Target	연구분야	Chemical Structure

HY-13012

RepSox Maximum Cited Publications 21 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-78349

A 77-01 2 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-18758

IN-1130 1 Publications Verification	TGF-β Receptor	Inflammation/Immunology Cancer
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 .

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-128437

TGFβ-IN-5 1 Publications Verification	TGF-β Receptor	Inflammation/Immunology
TGFβ-IN-5 is a type I transforming growth factor-β receptor (TGF-β R1) kinase inhibitor with an IC₅₀ value of 0.0485 μM. TGFβ-IN-5 reverses the effect of TGF-β-mediated cell activation on the expression of fibrosis-related genes. TGFβ-IN-5 can be used in the research of fibroproliferative diseases .

HY-13012R

RepSox (Standard) E-616452 (Standard); SJN 2511 (Standard)	Organoid TGF-β Receptor Reference Standards	Metabolic Disease
RepSox (Standard) is the analytical standard of RepSox. This product is intended for research and analytical applications. 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-W707119

RepSox hydrochloride E-616452 hydrochloride; SJN 2511 hydrochloride	TGF-beta/Smad Anaplastic lymphoma kinase (ALK)	Metabolic Disease
RepSox hydrochloride is a potent and selective inhibitor of transforming growth factor-β receptor I/activin-like kinase 5 (TGF-β-RI/ALK5). RepSox hydrochloride inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox hydrochloride can be used in the study of obesity and related metabolic diseases such as type 2 diabetes.

HY-18758R

IN-1130 (Standard)	TGF-β Receptor	Inflammation/Immunology Cancer
IN-1130 (Standard) is the analytical standard of IN-1130. This product is intended for research and analytical applications. 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 .

HY-13012S

RepSox-d5 E-616452-d₅; SJN 2511-d₅	Isotope-Labeled Compounds TGF-β Receptor	Metabolic Disease
RepSox-d₅ (E-616452-d₅) is the deuterium labeled RepSox (HY-13012). 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 .

Cat. No.	상품명

HY-L018

TGF-beta/Smad Compound Library	413 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 413 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

413 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 413 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.	상품명	Chemical Structure

HY-13012S

RepSox-d5
RepSox-d₅ (E-616452-d₅) is the deuterium labeled RepSox (HY-13012). 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 .

RepSox-d5

RepSox-d₅ (E-616452-d₅) is the deuterium labeled RepSox (HY-13012). 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 .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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