SB505124

For research use only.

Catalog No.S2186

25 publications

SB505124 Chemical Structure

CAS No. 694433-59-5

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.

Selleck's SB505124 has been cited by 25 publications

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.
Targets
ALK5 [1]
(Cell-free assay)
ALK4 [1]
(Cell-free assay)
47 nM 129 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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Sf9 M331TGZ2dmO2aX;uJIF{e2G7 NGi3d21KdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IFfTWE1nfXOnZDDBUGs2KGW6cILld5Nm\CCrbjDT[lkh[2WubIOgeZNqdmdiY3Hz[YlvKGG|IHGgd5Vje3S{YYTlJIJ6KHKjZHnvbZNwfG:yaXOgdJJwfGWrbjDrbY5ie2ViYYPzZZktKEmFNUC9NE4xPTR2zszN Mnq2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyNEeyNlYoRjJ|MES3NlI3RC:jPh?=
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A673 MlWwdWhVWyCjc4PhfS=> M3LuZZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGE3PzNiY3XscJMq MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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fibroblast cells MlradWhVWyCjc4PhfS=> M4qwT5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJINwdnS{b3ygTIghf2muZDD0fZBmKG[rYoLvZoxie3RiY3XscJM> NX;sZZh2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-SMAD2 / SMAD2 / Cleaved PARP / ZEB1 / Snail ; 

PubMed: 30401983     


Phosphorylation of SMAD2 was reduced in a dose-dependent manner in WERI Rb1 (a), Y79 (b), HSJD-RBVS-10 (c) cells treated with SB505124 for 4 days at the indicated doses, as found by Western blot. Induction of cleaved PARP, indicative of apoptosis, and reduction in Snail and ZEB1 protein levels were also observed, starting at the dose of 2 μM. No phosphorylation of SMAD3 was detected in these lines, while a dose-dependent decrease in the protein levels of SMAD3 was observed in WERI Rb1 and Y79 (Figure 4a-b, bottom panel). PANC-1 cells treated with TGF-β1 at 10 ng/mL for 2 hours were used as positive control for phospho-SMAD3 antibody.

30401983
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.
Cell Research:[1]
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  • Cell lines: A498, FaO and NRP 154 cells
  • Concentrations: 0-10 μM
  • Incubation Time: 48 hours
  • Method: Cell viability is measured as described by Laping et al., 2002 or by using the modified tetrazolium salt WST-1. XTT assay: The cells are serum-deprived for 24 hours and then treated with SB505124 for 48 hours to assess the cellular toxicity. Cell viability is determined by incubating cells for 4 hours with XTT labeling and electron coupling reagent according to the manufacturer's directions. Live cells with active mitochondria produce an orange-colored product, formazan, which is detected using a plate reader at between A450 nm and A500 nm with a reference wavelength greater than 600 nm. The absorbance values correlate with the number of viable cells. Modified tetrazolium salt WST-1: Approximately 2000 cells are seeded in 96-well dishes in 100 μL of 0.2% FBS phenol red-free media overnight. The cells are treated with 50 μL of SB505124 (to achieve the final concentrations indicated) for 30 minutes before being treated with or without TGF-β1 and TNF-α to a final volume of 200 μL. Cell growth is measured at the indicated time points by incubating each well with 10 μL of WST-1 for 3 hours at 37 °C. Metabolically active cells cleave WST-1 to water-soluble formazan, which is directly quantitated with an enzyme-linked immunosorbent assay plate reader. Each experiment is done at least twice, and treatment for each cell line is done in triplicate.
    (Only for Reference)
Animal Research:[5]
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  • Animal Models: New Zealand White (NZW) rabbits after glaucoma filtration surgery (GFS).
  • Dosages: Tablets containing 5 mg of SB505124.
  • Administration: Administered via p.o.
    (Only for Reference)

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(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
Formula

C20H21N3O2

CAS No. 694433-59-5
Storage powder
in solvent
Synonyms N/A
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)
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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID