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SB505124
Catalog No.S2186
For research use only.
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.
CAS No. 694433-59-5
Selleck's SB505124 has been cited by 28 publications
Purity & Quality Control
Choose Selective TGF-beta/Smad Inhibitors
Related Compound Libraries
Other TGF-beta/Smad Products
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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| Targets |
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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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| Cell Data |
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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 (from reference)
| Kinase Assay:[1] |
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|---|---|
| Cell Research:[1] |
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| Animal Research:[5] |
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| References |
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Solubility (25°C)
|
In vitro |
DMSO |
67 mg/mL
(199.76 mM) |
| Ethanol |
67 mg/mL
(199.76 mM) |
|
| Water |
Insoluble
|
|
|
In vivo |
Add solvents to the product individually and in order |
7.5 mg/mL |
Chemical Information
| Molecular Weight | 335.4 | ||
|---|---|---|---|
| Formula | C20H21N3O2 |
||
| CAS No. | 694433-59-5 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CC1=NC(=CC=C1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=C(C=C3)OCO4 | ||
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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%
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% ddH2O
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Calculation results:
Working concentration: mg/ml;
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 ddH2O, 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.
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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