SB505124 |
Catalog No.GC13769
One-Click Copy Product Info
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SB505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50 values of 129nM and 47nM for ALK4, ALK5, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 694433-59-5
Sample solution is provided at 25 µL, 10mM.
SB505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50 values of 129nM and 47nM for ALK4, ALK5, respectively[1]. SB505124 can inhibit the Wnt and TGF-β1 signaling pathways, reduce inflammatory responses, and decrease the levels of fibrosis markers (such as collagen, α-SMA and fibronectin)[2]. SB505124 has been widely used to inhibit the differentiation of Th17 cells and regulate inflammation in mouse models of arthritis[3].
In vitro, SB505124 treatment at 3μM for 10 days significantly inhibited the osteogenic differentiation of human bone marrow mesenchymal stem cells (hBMSCs), reduced the formation of mineralized matrix, and downregulated osteogenic-related genes[4]. Treatment with SB505124 (2.5μM) for 24 hours significantly enhanced the sensitivity of doxorubicin (DTX)-resistant DU 145 cells to DTX and induced cell death[5]. Pretreatment of rabbit conjunctival submucosal fibroblasts with 10µM SB505124 for 1 hour significantly reduced the level of pSmad2 induced by TGF-β2 as well as the expressions of CTGF and α-SMA[6].
In vivo, SB505124 treatment via intraperitoneal injection at a dose of 10mg/kg once every 12 hours for 5 days alleviated the extent of tertiary neurodegeneration and blood-brain barrier dysfunction in the perinatal mouse model with hypoxic-ischemic brain injury, and improved sensory-motor deficits[7]. SB505124 treatment for 2 weeks (5mg/kg/day; i.p.) caused the increase of erythrocytes in the peripheral blood and the normalized proportion of erythroblast cell clusters in the Lewis lung carcinoma (LLC) cell-xenograft mouse models[8].
References:
[1] Byfield S D C, Major C, Laping N J, et al. SB-505124 is a selective inhibitor of transforming growth factor-β type I receptors ALK4, ALK5, and ALK7[J]. Molecular pharmacology, 2004, 65(3): 744-752.
[2] Tang Y, Liu J, Liu L. Angiotensin-converting Enzyme 2 Suppresses Pulmonary Fibrosis Associated with Wnt and TGF-β1 Signaling Pathways[J]. Discovery medicine, 2024, 36(190): 2274-2286.
[3] Aarts J, Van Caam A, Helsen M, et al. Ab0082 Inhibition Of Tgfβ Signaling Using Sb-505124 Blocks Th17 Differentiation And Restores The Th17/Treg Balance In Vivo, But Does Not Suppress Experimental Arthritis[J]. Annals of the Rheumatic Diseases, 2020, 79: 1341.
[4] Almuraikhi N. Inhibition of TGF‐β type I receptor by SB505124 down‐regulates osteoblast differentiation and mineralization of human mesenchymal stem cells[J]. Cell Biochemistry and Function, 2023, 41(5): 564-572.
[5] Li Y, Zhang B, Xiang L, et al. TGF-β causes docetaxel resistance in prostate cancer via the induction of Bcl-2 by acetylated KLF5 and protein stabilization[J]. Theranostics, 2020, 10(17): 7656.
[6] Sapitro J, Dunmire J J, Scott S E, et al. Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by activin receptor-like kinase 5 inhibitor[J]. Molecular Vision, 2010, 16: 1880.
[7] Kanal H D, Levison S W. Neuroprotective effects of delayed TGF-β1 receptor antagonist administration on perinatal hypoxic-ischemic brain injury[J]. Developmental Neuroscience, 2024, 46(3): 188-200.
[8] Wang B, Wang Y, Chen H, et al. Inhibition of TGFβ improves hematopoietic stem cell niche and ameliorates cancer-related anemia[J]. Stem Cell Research & Therapy, 2021, 12(1): 65.
| Cell experiment [1]: | |
Cell lines | Human bone marrow mesenchymal stem cells (hBMSCs) |
Preparation Method | Human bone marrow mesenchymal stem cells (hBMSCs) were cultured in Dulbecco's Modified Eagle Medium (DMEM), supplemented with 4500mg/l D-glucose, 4mM L-glutamine, 110mg/l 10% sodium pyruvate, 10% fetal bovine serum (FBS), 1% non-essential amino acids, and 1% penicillin-streptomycin. The incubator temperature was set at 37°C, humidity at 95%, and CO2 concentration at 5% to maintain cell growth. The cells were seeded in 96-well plates, with 300μl of culture medium added to each well, and 0.3, 3, and 30μM of SB505124 were added respectively. The control group cells were added with DMSO. After 72h, cell viability was analyzed. |
Reaction Conditions | 0.3, 3, and 30μM; 72h |
Applications | SB505124 treatment significantly decreased the cell viability of U87MG cells at 30μM. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | The C57BL/6 mice were raised in a standard environment and were allowed to freely consume food and water. 2×106 LLC cells were suspended in 100μl of sterile PBS, or an equal volume of PBS solution was injected subcutaneously into the left abdomen of 8-week-old male mice. From the 7th day to the 21st day after tumor implantation, 5mg/kg doses of SB505124 or DMSO were injected intraperitoneally daily. Under anesthesia, blood samples were drawn from the inferior vena cava of the mice for analysis. |
Dosage form | 5mg/kg/day for 2 weeks; i.p. |
Applications | SB505124 treatment attenuated the symptoms of cancer-related anemia in the LLC cell-xenograft mouse models. |
References: | |
| Cas No. | 694433-59-5 | SDF | |
| Chemical Name | 2-[4-(1,3-benzodioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl]-6-methylpyridine | ||
| Canonical SMILES | CC1=CC=CC(=N1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=C(C=C3)OCO4 | ||
| Formula | C20H21N3O2 | M.Wt | 335.4 |
| Solubility | ≥ 33.5mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9815 mL | 14.9076 mL | 29.8151 mL |
| 5 mM | 596.3 μL | 2.9815 mL | 5.963 mL |
| 10 mM | 298.2 μL | 1.4908 mL | 2.9815 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)