SB505124
For research use only.
Catalog No.S2186
15 publications
Molecular Weight(MW): 335.4
SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM in cell-free assays, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6.
7 Customer Reviews
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(D): Fluorescence micrographs of SOX2/FOXA2 double-staining of the conditions mentioned above. The TGF-b inhibitor SB-505124 (1 mM) was additionally used together with the complete medium. Nuclei were counterstained with DAPI. Original magnification 310 or 340. Abbreviations: DAPI, 40,6-diamidino-2-phenylindole; RA, retinoic acid.
Stem Cells, 2016, 34:2635-2647.. SB505124 purchased from Selleck.
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Primary chondrocytes isolated from Cre-negative mice were pretreated with 1 μM SB-505124 for 30 min, followed by an additional 30 min incubation of 10 ng/ml TGF-β1, 10 μM H89/1 μM SB-505124, or a combination of both. Western blotting was performed to detect the pCREB protein expressions. Quantitative data were shown in the right panel (two-way ANOVA followed by Tukey’s test, n = 4 mice per group).
Osteoarthritis Cartilage, 2017, 25(11):1868-1879. SB505124 purchased from Selleck.
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FCS confirmed that SCH772984, SB505124 and Verteporfin administration apparently reduced the CD44 expression
Oncotarget, 2016, 7(47):77495-77507. SB505124 purchased from Selleck.
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(C) The CTX-II release from the ECM of chondrocytes treated with/without 10 nM 1α,25(OH)2D3, TNF-α and TGF-β receptor inhibitor (SB505124). The effects of 1α,25(OH)2D3 on TNF-α stimulated chondrocytes were contracted by TGF-β receptor inhibitor. Values are the means ± 95% CI.
Osteoarthritis Cartilage, 2016, 24(2):345-53. SB505124 purchased from Selleck.
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Expression of NKILA assayed by qRT-PCR in A549 and H226 cells induced by TGF-β1 with or without TGF-β or NF-κB inhibition by SB505124 (SB) and JSH-23 (JSH) respectively.
J Exp Clin Cancer Res, 2017, 36(1):54. SB505124 purchased from Selleck.
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TGF-b1 stimulates vimentin expression via Smad-signaling in U937 cells. Cells were stimulated with rhTGFb1 (0.2 ng/ml) after pretreatment with 0.2 nM SB505124 (an inhibitor of Smad2/3 phosphorylation) or 5 nM wortmannin (a PI3 K inhibitor). Total cell lysates was separated by SDS-PAGE and immunoblots were analyzed by Western blot. Cells without treatment belong to the control group. Histograms show the ratios of proteins to GAPDH. # p < 0.05 and ## P < 0.01 vs. the control group. ** P < 0.01 vs. the group treated with TGF-b1 alone
Biomed Pharmacother, 2016, 83:1132-1140. SB505124 purchased from Selleck.
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Total cell lysates was separated by SDS-PAGE and immunoblots were analyzed with specific antibodies after treatment with signaling inhibitors (0.2 nM SB505124, an inhibitor of Smad2/3 phosphorylation; 5 nM wortmannin, a PI3K inhibitor) for 30 min, cells were stimulated with rhTGF-β1 (0.2 ng/mL). Cells without treatment belong to the control group.
Am J Chin Med, 2015, 43(1):183-98. SB505124 purchased from Selleck.
Purity & Quality Control
Choose Selective TGF-beta/Smad Inhibitors
Biological Activity
| Description | SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM in cell-free assays, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6. | |||||||||||||||||||||||||||||||||||||
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| In vitro |
SB505124 is identified as a reversible ATP competitive and selective ALK inhibitor of ALK4 and ALK5. SB505124 shows no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 hours, and blocks TGF-β–induced apoptosis of FaO cells and NRP 154 cells in a concentration-dependent manner. [1] In human umbilical vein endothelial cells (HUVEC), SB505124 (500 nM) blocks the changes of TGF-β1 on F-actin assembly and prevents ROS production induced by TGF-β. [2] By inhibiting TGF-beta1 signaling, SB505124 leads to decreased deferoxamine (DFO)-induced neurogenesis. [3] A recent study shows that SB505124 suppresses the migration and invasion of breast cancer MCF-7-M5 cells. [4] |
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| Assay |
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| In vivo | In a rabbit GFS model, SB505124 decreased the intraocular pressure (IOP) levels and reduces subconjunctival cell infiltration and scarring at the surgical site in the GFS. [5] In tacrolimus (TAC)-treated mice and FK12EC KO mice, SB505124 prevents the activation of endothelial TGF-β receptors and induction of renal arteriolar hyalinosis. [6] |
Protocol
| Kinase Assay:[1] |
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In Vitro Protein Kinase Assay : Kinase assays are performed as described by Laping et al., 2002 using the kinase domain of ALK5 and full-length N-terminal fused GST-Smad3. Kinase assays are performed with 65 nM GST-ALK5 and 184 nM GST-Smad3 in 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 1 mM dithiothreitol, and 3 μM ATP. Reactions are incubated with 0.5 μCi of [33P]γATP for 3 hours at 30 °C. Phosphorylated protein is captured on P-81 paper , washed with 0.5% phosphoric acid, and counted by liquid scintillation. Alternatively, Smad3 or Smad1 protein is also coated onto FlashPlate Sterile Basic Microplates. Kinase assays are then performed in FlashPlates with same assay conditions using either the kinase domain of ALK5 with Smad3 as substrate or the kinase domain of ALK6 (BMP receptor) with Smad1 as substrate. Plates are washed three times with phosphate buffer and counted by TopCount. |
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| Cell Research:[1] |
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| Animal Research:[5] |
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Solubility (25°C)
| In vitro | DMSO | 67 mg/mL (199.76 mM) |
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| Water | Insoluble | |
| Ethanol | '''67 mg/mL | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5%DMSO+40%PEG300+5%Tween80+50%ddH2O For best results, use promptly after mixing. |
7.5 mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 335.4 |
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| Formula | C20H21N3O2 |
| CAS No. | 694433-59-5 |
| Storage |
powder in solvent |
| Synonyms | N/A |
| Smiles | CC1=CC=CC(=N1)C2=C(N=C([NH]2)C(C)(C)C)C3=CC4=C(OCO4)C=C3 |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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.
Bio Calculators
Molarity Calculator
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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