Art. -Nr.: HY-13521

SB-505124

24 Cited Publications

Kundenbewertung

Based on 24 publication(s) in Google Scholar

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.

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Reinheit: 99.73%
CAS. Nr.: 694433-59-5
Formel: C₂₀H₂₁N₃O₂
Molecular Weight:335.40

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SB-505124 Chemical Structure

CAS. Nr.: 694433-59-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (24)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 129 nM (ALK4), 47 nM (ALK5)

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	0.0766 μM Compound: 1, SB-5051124	Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay	[PMID: 24786585]
HaCaT	IC₅₀	0.0438 μM Compound: 1, SB-5051124	Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay	[PMID: 24786585]
Sf9	IC₅₀	0.054 μM Compound: 1, SB-5051124	Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay	[PMID: 24786585]
Sf9	IC₅₀	0.054 μM Compound: 1, SB-505124	Inhibition of GST-fused recombinant human ALK5 expressed in baculovirus-infected insect Sf9 cells using casein as substrate by radioisotope-based assay Inhibition of GST-fused recombinant human ALK5 expressed in baculovirus-infected insect Sf9 cells using casein as substrate by radioisotope-based assay	[PMID: 24704197]
Sf9	IC₅₀	0.054 μM Compound: 2, SB-505124	Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells	[PMID: 21435890]
Sf9	IC₅₀	0.169 μM Compound: 2, SB-505124	Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells	[PMID: 20472445]
Sf9	IC₅₀	34.9 nM Compound: 1; SB-505124	Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay	[PMID: 26483198]
Sf9	IC₅₀	54.4 nM Compound: 1, SB-505124	Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells using casein as a substrate by radioisotopic protein kinase assay Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells using casein as a substrate by radioisotopic protein kinase assay	[PMID: 23047226]

In Vitro

SB-505124 demonstrates no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC₅₀ value of 129±11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 μM. SB-505124 (1 μM) inhibits the TGF-β-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB-505124 (1 or 5 μM) potently inhibits TGF-β-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells^[1]. SB-505124 (10 μM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro^[2]. SB-505124 susspresses CTGF and α-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB-505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SB-505124 (5 mg/kg; i.p.) alone has no effect in C57Bl6 mice with A549 xenografts, but administration of SB-505124 with a single dose of Carboplatin (60 mg/kg) results in durable responses without the need for maintenance therapy in five animals^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57Bl6 mice with A549 xenografts^[4]
Dosage:

5 mg/kg
Administration:

I.p.; daily
Result:

Had no effect alone, but administration with a single dose of carboplatin (60 mg/kg) resulted in durable responses without the need for maintenance therapy in five animals.

Chemical Information

CAS. Nr. 694433-59-5
Appearance Solid
Molecular Weight 335.40
Formel C₂₀H₂₁N₃O₂
Color White to off-white
SMILES

CC1=CC=CC(C2=C(C3=CC=C(OCO4)C4=C3)N=C(C(C)(C)C)N2)=N1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (24)

All IFWB

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Journal Impact Factor

Cancer Cell

Integrated single-cell and spatial transcriptomics uncover distinct cellular subtypes involved in neural invasion in pancreatic cancer. [Abstract]

2025 Jul 17:S1535-6108(25)00270-3. PMID: 40680743
Nat Metab

HK1 from hepatic stellate cell-derived extracellular vesicles promotes progression of hepatocellular carcinoma. [Abstract]

2022 Oct;4(10):1306-1321. PMID: 36192599
Bone Res

Collagen type II suppresses articular chondrocyte hypertrophy and osteoarthritis progression by promoting integrin β1-SMAD1 interaction. [Abstract]

2019 Mar 6;7:8. PMID: 30854241
Exp Mol Med

Circular RNA CREBBP modulates cartilage degradation by activating the Smad1/5 pathway through the TGFβ2/ALK1 axis. [Abstract]

2022 Oct;54(10):1727-1740. PMID: 36224344
ACS Nano

Tumor Microenvironment-Activatable Nanosystem Capable of Overcoming Multiple Therapeutic Obstacles for Augmenting Immuno/Metal-Ion Therapy. [Abstract]

2024 Mar 26;18(12):8996-9010. PMID: 38477219
ACS Nano

Self-Delivery Ternary Bioregulators for Photodynamic Amplified Immunotherapy by Tumor Microenvironment Reprogramming. [Abstract]

2022 Jan 25;16(1):1182-1197. PMID: 35023720
J Nanobiotechnology

2026 Apr 11;24(1):480.
Adv Sci (Weinh)

Genetically Engineered Hematopoietic Stem Cells Deliver TGF-β Inhibitor to Enhance Bone Metastases Immunotherapy. [Abstract]

2022 Oct;9(28):e2201451. PMID: 35948516
Cell Death Dis

Activation of AKT via a dual mechanism enhances the susceptibility of melanoma cells to glucose deprivation. [Abstract]

2025 Aug 7;16(1):595. PMID: 40774947
Adv Healthc Mater

Multifunctional ICG-SB@Lip-ZA Nanosystem Focuses on Remodeling the Inflammatory-Immunosuppressive Microenvironment After Photothermal Therapy to Potentiate Cancer Photothermal Immunotherapy. [Abstract]

2024 Oct 23:e2402211. PMID: 39440627
Genome Med

Single-cell transcriptomics reveal distinct immune-infiltrating phenotypes and macrophage-tumor interaction axes among different lineages of pituitary neuroendocrine tumors. [Abstract]

2024 Apr 24;16(1):60. PMID: 38658971
Oncogene

ACVR1C/SMAD2 signaling promotes invasion and growth in retinoblastoma. [Abstract]

2019 Mar;38(12):2056-2075. PMID: 30401983

SB-505124 purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Mar;38(12):2056-2075. [Abstract]

Treatment with SB505124 for 3 days significantly increases apoptosis at 4 and 8 μM in WERI Rb1.

SB-505124 purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Mar;38(12):2056-2075. [Abstract]

Treatment with SB505124 for 3 days significantly increases apoptosis at 4 and 8 μM in WERI Rb1.

SB-505124 purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Mar;38(12):2056-2075. [Abstract]

The effects on growth and invasion are paralleled by a dose-dependent inhibition in SMAD2 phosphorylation upon treatment with SB505124 at 0.5, 1, 2, 3, 4, 8 μM for 4 days.
EMBO J

BMP4 initiates and patterns ventral-caudal structures in zebrafish and human pluripotent stem cell aggregates. [Abstract]

2025 Nov 24. PMID: 41286028
J Genet Genomics

Cdx1b protects intestinal cell fate by repressing signaling networks for liver specification. [Abstract]

2022 Dec;49(12):1101-1113. PMID: 36460297
J Cell Mol Med

Sinomenine Ameliorated Microglial Activation and Neuropathic Pain After Chronic Constriction Injury Via TGF-β1/ALK5/Smad3 Signalling Pathway. [Abstract]

2024 Nov;28(22):e70214. PMID: 39586784
iScience

Amphiregulin orchestrates the paracrine immune-suppressive function of amniotic-derived cells through its interplay with COX-2/PGE2/EP4 axis. [Abstract]

2024 Jul 14;27(8):110508. PMID: 39156643
J Cell Physiol

LncRNA-ATB promotes TGF-β-induced glioma cells invasion through NF-κB and P38/MAPK pathway. [Abstract]

2019 Dec;234(12):23302-23314. PMID: 31140621
Development

Nodal and Hedgehog synergize in gill slit formation during development of the cephalochordate Branchiostoma floridae. [Abstract]

2018 Aug 6;145(15). pii: dev162586. PMID: 29980563
J Funct Foods

2021, 104403.
Cytokine

Platelet TGF-β1 inhibits the migration and proliferation of smooth muscle cells in aneurysms. [Abstract]

2022 Oct:158:155969. PMID: 35930963
Regen Med

Mesenchymal stem cell-derived neural progenitors attenuate proinflammatory microglial activation via paracrine mechanisms. [Abstract]

2023 Mar;18(3):259-273. PMID: 36852422
Biomed Pharmacother

Transforming growth factor-β receptor I kinase plays a crucial role in oligodendrocyte regeneration after demyelination. [Abstract]

2025 May 1:187:118094. PMID: 40315672
J Bioma Ter Tiss Eng

2020 Jun.
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 113.33 mg/mL (337.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9815 mL

14.9076 mL

29.8151 mL

5 mM

0.5963 mL

2.9815 mL

5.9630 mL

10 mM

0.2982 mL

1.4908 mL

2.9815 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. DaCosta Byfield S, et al. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2004 Mar;65(3):744-52. [Content Brief]

[2]. Sutariya V, et al. Thermoreversible gel for delivery of receptor-like kinase 5 inhibitor SB-505124 for glaucoma filtration surgery. Pharm Dev Technol. 2013 Jul-Aug;18(4):957-62. [Content Brief]

[3]. Sapitro J, et al. Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by receptor-like kinase 5 inhibitor. Mol Vis. 2010 Sep 16;16:1880-92. [Content Brief]

[4]. Marini KD, et al. Inhibition of activin signaling in lung adenocarcinoma increases the therapeutic index of platinum chemotherapy. Sci Transl Med. 2018 Jul 25;10(451). pii: eaat3504. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9815 mL	14.9076 mL	29.8151 mL	74.5379 mL
	5 mM	0.5963 mL	2.9815 mL	5.9630 mL	14.9076 mL
	10 mM	0.2982 mL	1.4908 mL	2.9815 mL	7.4538 mL
	15 mM	0.1988 mL	0.9938 mL	1.9877 mL	4.9692 mL
	20 mM	0.1491 mL	0.7454 mL	1.4908 mL	3.7269 mL
	25 mM	0.1193 mL	0.5963 mL	1.1926 mL	2.9815 mL
	30 mM	0.0994 mL	0.4969 mL	0.9938 mL	2.4846 mL
	40 mM	0.0745 mL	0.3727 mL	0.7454 mL	1.8634 mL
	50 mM	0.0596 mL	0.2982 mL	0.5963 mL	1.4908 mL
	60 mM	0.0497 mL	0.2485 mL	0.4969 mL	1.2423 mL
	80 mM	0.0373 mL	0.1863 mL	0.3727 mL	0.9317 mL
	100 mM	0.0298 mL	0.1491 mL	0.2982 mL	0.7454 mL

Keywords

SB-505124

24 Cited Publications

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SB-505124

Kinase Inhibitor Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Colorectal Cancer Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SB-505124

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SB-505124

Kinase Inhibitor Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Colorectal Cancer Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SB-505124

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SB-505124 Related Classifications

HY-13521 Related Classifications