SB-505124 hydrochloride
Based on 23 publication(s) in Google Scholar
SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptor (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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- Purity: 98.52%
- CAS No.: 356559-13-2
- 화학식: C20H22ClN3O2
- 분자량:371.86
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SB-505124 hydrochloride
More- Cancer Cell. 2025 Jul 17:S1535-6108(25)00270-3. [Abstract]
- Nat Metab. 2022 Oct;4(10):1306-1321. [Abstract]
- ACS Nano. 2024 Mar 26;18(12):8996-9010. [Abstract]
- ACS Nano. 2022 Jan 25;16(1):1182-1197. [Abstract]
- Bone Res. 2019 Mar 6;7:8. [Abstract]
- Adv Sci (Weinh). 2022 Oct;9(28):e2201451. [Abstract]
- Exp Mol Med. 2022 Oct;54(10):1727-1740. [Abstract]
- Genome Med. 2024 Apr 24;16(1):60. [Abstract]
- Cell Death Dis. 2025 Aug 7;16(1):595. [Abstract]
- Adv Healthc Mater. 2024 Oct 23:e2402211. [Abstract]
- EMBO J. 2025 Nov 24. [Abstract]
- Biomed Pharmacother. 2025 May 1:187:118094. [Abstract]
- Oncogene. 2019 Mar;38(12):2056-2075. [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 Funct Foods. 2021, 104403.
- J Cell Physiol. 2019 Dec;234(12):23302-23314. [Abstract]
- Cytokine. 2022 Oct:158:155969. [Abstract]
- Development. 2018 Aug 6;145(15). pii: dev162586. [Abstract]
- Regen Med. 2023 Mar;18(3):259-273. [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
Biological Activity
IC50: 129 nM (ALK4), 47 nM (ALK5)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
0.054 μM
Compound: 1, SBe505124
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Inhibition of human recombinant GST-fused ALK5 expressed in insect Sf9 cells using casein as substrate by radiometric kinase assay
Inhibition of human recombinant GST-fused ALK5 expressed in insect Sf9 cells using casein as substrate by radiometric kinase assay
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[PMID: 21696866] |
| 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: 21911290] |
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.
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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CAS No. 356559-13-2
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Appearance Solid
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분자량 371.86
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화학식 C20H22ClN3O2
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Color Light yellow to green yellow
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SMILES
CC1=CC=CC(C2=C(C3=CC=C(OCO4)C4=C3)N=C(C(C)(C)C)N2)=N1.[H]Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (23)
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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 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 -
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 -
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 -
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 -
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 -
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 -
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 -
EMBO J
BMP4 initiates and patterns ventral-caudal structures in zebrafish and human pluripotent stem cell aggregates. [Abstract]2025 Nov 24. PMID: 41286028 -
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 -
Oncogene
2019 Mar;38(12):2056-2075. PMID: 30401983
SB-505124 hydrochloride 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 hydrochloride 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 hydrochloride 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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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 -
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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 -
Cytokine
Platelet TGF-β1 inhibits the migration and proliferation of smooth muscle cells in aneurysms. [Abstract]2022 Oct:158:155969. PMID: 35930963 -
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 -
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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용액&용해도
Methanol : 125 mg/mL (336.15 mM; Need ultrasonic)
DMSO : 50 mg/mL (134.46 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (6.72 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.72 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
순도&문서
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Data Sheet (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Methanol | 1 mM | 2.6892 mL | 13.4459 mL | 26.8918 mL | 67.2296 mL |
| 5 mM | 0.5378 mL | 2.6892 mL | 5.3784 mL | 13.4459 mL | |
| 10 mM | 0.2689 mL | 1.3446 mL | 2.6892 mL | 6.7230 mL | |
| 15 mM | 0.1793 mL | 0.8964 mL | 1.7928 mL | 4.4820 mL | |
| 20 mM | 0.1345 mL | 0.6723 mL | 1.3446 mL | 3.3615 mL | |
| 25 mM | 0.1076 mL | 0.5378 mL | 1.0757 mL | 2.6892 mL | |
| 30 mM | 0.0896 mL | 0.4482 mL | 0.8964 mL | 2.2410 mL | |
| 40 mM | 0.0672 mL | 0.3361 mL | 0.6723 mL | 1.6807 mL | |
| 50 mM | 0.0538 mL | 0.2689 mL | 0.5378 mL | 1.3446 mL | |
| 60 mM | 0.0448 mL | 0.2241 mL | 0.4482 mL | 1.1205 mL | |
| 80 mM | 0.0336 mL | 0.1681 mL | 0.3361 mL | 0.8404 mL | |
| 100 mM | 0.0269 mL | 0.1345 mL | 0.2689 mL | 0.6723 mL |
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