1. TGF-beta/Smad
  2. TGF-β Receptor

SB-505124 

Cat. No.: HY-13521 Purity: 99.73%
Handling Instructions

SB-505124 is a selective inhibitor of TGFβR with IC50 of 129 nM and 47 nM for ALK4, ALK5, respectively, and it does not inhibits ALK1, 2, 3, or 6 but ALK7.

For research use only. We do not sell to patients.

SB-505124 Chemical Structure

SB-505124 Chemical Structure

CAS No. : 694433-59-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 158 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 504 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
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Other Forms of SB-505124:

  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

SB-505124 is a selective inhibitor of TGFβR with IC50 of 129 nM and 47 nM for ALK4, ALK5, respectively, and it does not inhibits ALK1, 2, 3, or 6 but ALK7.

IC50 & Target

IC50: 129 nM (ALK4), 47 nM (ALK5)

In Vitro

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].

Solvent & Solubility
In Vitro: 

DMSO : 113.33 mg/mL (337.90 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9815 mL 14.9076 mL 29.8151 mL
5 mM 0.5963 mL 2.9815 mL 5.9630 mL
10 mM 0.2982 mL 1.4908 mL 2.9815 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Briefly, phospho-p38 is immunoprecipitated from 200 μg of cell lysates with an immobilized phosphor-p38 antibody overnight at 4°C. p38 kinase activity is measured using 2 μg of ATF-2 fusion protein as the substrate with addition of 200 μM ATP. After a 30-min incubation at 30°C, the reaction is terminated with LaemmLi sample buffer, and the proteins are boiled and resolved by 10% SDS-polyacrylamide gel electrophoresis, transferred to nitrocellulose membrane, and immunoblotted with phospho-ATF-2 antibody.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Cell viability is measured as described previously or by using the 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 SB-505124 (to achieve the final concentrations indicated) for 30 min 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 h 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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

335.40

Formula

C₂₀H₂₁N₃O₂

CAS No.

694433-59-5

SMILES

CC1=CC=CC(C2=C(C3=CC=C(OCO4)C4=C3)N=C(C(C)(C)C)N2)=N1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
SB-505124
Cat. No.:
HY-13521
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SB-505124

Cat. No.: HY-13521