SB-505124
Based on 27 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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.73%
- No. CAS: 694433-59-5
- Fòrmula: C20H21N3O2
- Peso molecular:335.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SB-505124
More- Cancer Cell. 2025 Sep 8;43(9):1656-1676.e10. [Abstract]
- Cell. 2026 Sep 14:S0092-8674(26)01003-2.
- Nat Metab. 2022 Oct;4(10):1306-1321. [Abstract]
- Bone Res. 2019 Mar 6:7:8. [Abstract]
- Exp Mol Med. 2022 Oct;54(10):1727-1740. [Abstract]
- ACS Nano. 2024 Mar 26;18(12):8996-9010. [Abstract]
- ACS Nano. 2022 Jan 25;16(1):1182-1197. [Abstract]
- J Nanobiotechnology. 2026 Apr 11;24(1):480.
- Adv Sci (Weinh). 2022 Oct;9(28):e2201451. [Abstract]
- Cell Death Dis. 2025 Aug 7;16(1):595. [Abstract]
- Adv Healthc Mater. 2025 Jan;14(1):e2402211. [Abstract]
- Genome Med. 2024 Apr 24;16(1):60. [Abstract]
- Oncogene. 2019 Mar;38(12):2056-2075. [Abstract]
- EMBO J. 2025 Nov 24. [Abstract]
- J Genet Genomics. 2022 Dec;49(12):1101-1113. [Abstract]
- J Cell Mol Med. 2024 Nov;28(22):e70214. [Abstract]
- iScience. 2024 Jul 14;27(8):110508. [Abstract]
- J Cell Physiol. 2019 Dec;234(12):23302-23314. [Abstract]
- Development. 2018 Aug 6;145(15):dev162586. [Abstract]
- J Funct Foods. 2021, 104403.
- Cytokine. 2022 Oct:158:155969. [Abstract]
- Exp Eye Res. 2026 Aug 19:272:111211.
- Regen Med. 2023 Mar;18(3):259-273. [Abstract]
- University of Colorado Anschutz Medical Campus. 2026.
- Biomed Pharmacother. 2025 Jun:187:118094. [Abstract]
- J Bioma Ter Tiss Eng. 2020 Jun.
- Patent. US20180263995A1.
Customer Validation & Images
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IF
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IF
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WB
Actividad biológica
Descripciòn
IC50 & Target
IC50: 129 nM (ALK4), 47 nM (ALK5)
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| 4T1 | IC50 |
0.0766 μM
Compound: 1, SB-5051124
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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
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[PMID: 24786585] |
| HaCaT | IC50 |
0.0438 μM
Compound: 1, SB-5051124
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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
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[PMID: 24786585] |
| Sf9 | IC50 |
0.054 μM
Compound: 1, SB-5051124
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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
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[PMID: 24786585] |
| Sf9 | IC50 |
0.054 μM
Compound: 1, SB-505124
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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
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[PMID: 24704197] |
| Sf9 | IC50 |
0.054 μM
Compound: 2, SB-505124
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Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells
Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells
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[PMID: 21435890] |
| Sf9 | IC50 |
0.169 μM
Compound: 2, SB-505124
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Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells
Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells
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[PMID: 20472445] |
| Sf9 | IC50 |
34.9 nM
Compound: 1; SB-505124
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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
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[PMID: 26483198] |
| Sf9 | IC50 |
54.4 nM
Compound: 1, SB-505124
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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
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[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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl6 mice with A549 xenografts[4]
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Dosage:5 mg/kg
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Administration:I.p.; daily
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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
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No. CAS 694433-59-5
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Appearance Solid
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Peso molecular 335.40
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Fòrmula C20H21N3O2
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Color White to off-white
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SMILES
CC1=CC=CC(C2=C(C3=CC=C(OCO4)C4=C3)N=C(C(C)(C)C)N2)=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (27)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Integrated single-cell and spatial transcriptomics uncover distinct cellular subtypes involved in neural invasion in pancreatic cancer. [Abstract]2025 Sep 8;43(9):1656-1676.e10. PMID: 40680743 -
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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 -
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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]2025 Jan;14(1):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
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.
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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):dev162586. PMID: 29980563 -
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Cytokine
Platelet TGF-β1 inhibits the migration and proliferation of smooth muscle cells in aneurysms. [Abstract]2022 Oct:158:155969. PMID: 35930963 -
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Regen Med
Mesenchymal stem cell-derived neural progenitors attenuate proinflammatory microglial activation via paracrine mechanisms. [Abstract]2023 Mar;18(3):259-273. PMID: 36852422 -
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Biomed Pharmacother
Transforming growth factor-β receptor I kinase plays a crucial role in oligodendrocyte regeneration after demyelination. [Abstract]2025 Jun:187:118094. PMID: 40315672 -
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Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (281 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
SB-505124 Related Classifications
HY-13521 Related Classifications
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