Product Categories

SB 525334

SB 525334 is a potent and selective inhibitor of TGF-β1 (ALK5) with IC50 of 14.3 nM.

Catalog No.S1476
5 5 1 Reviews 2 Product Citations
Price Stock Quantity  
USD 70 In stock
USD 120 In stock
USD 470 In stock
USD 870 In stock
Contact Us Bulk Inquiry Add to Wishlist

Free Overnight Delivery on all orders over $ 500.

Order now and get it on

Tel: +1-832-582-8158[email protected]

SB 525334 Chemical Structure
Molecular Weight: 343.42

Validation & Quality Control

Customer Reviews(1)

Quality Control & MSDS

Related Compound Libraries

SB 525334 is available in the following compound libraries:

Cambridge Cancer Compound Library(96-well) Chemical Library (96-well) Inhibitor Library (96-well) Kinase Inhibitor Library (96-well) Stem Cell Small Molecule Compound Library (96-well) Tyrosine Kinase Inhibitor Library (96-Well)

Product Information

  • Compare TGF-beta/Smad Inhibitors
    Compare TGF-beta/Smad Inhibitors
  • Research Area

Product Description

Biological Activity Protocol Chemical Information Customer Reviews Product Citations Tech Support & FAQs

Biological Activity

Description SB 525334 is a potent and selective inhibitor of TGF-β1 (ALK5) with IC50 of 14.3 nM.
Targets TGF-β1 (ALK5)
IC50 14.3 nM [1]
In vitro SB 525334 shows no inhibition in the enzymes ALK2, 3, and 6, with IC50 values > 10 μM. SB 525334 blocks phosphorylation induced by TGF-β1 and nuclear translocation of Smad2/3 in renal proximal tubule cells. SB 525334 also inhibits the increased mRNA expression levels of plasminogen activator inhibitor-1 (PAI-1) and procollagen α1(I) induced by TGF-β1 in A498 renal epithelial carcinoma cells at 1 μM). [1] SB 525334 (1 μM) attenuates the heightened sensitivity to TGF-β1 exhibited by pulmonary artery smooth muscle cells (PASMCs) from patients with familial forms of idiopathic pulmonary arterial hypertension (PAH). [2]
In vivo SB 525334 (10 mg/kg/day) decreases the renal mRNA levels of PAI-1, procollagen α1(I), and procollagen α1(III) in a nephritis-induced renal fibrosis rat model. Furthermore, PAN-induced proteinuria is significantly inhibited by SB 525334 (10 mg/kg/day). [1] SB 525334 may also be efficacious in mesenchymal tumors. SB 525334 (10 mg/kg/day) significantly decreases uterine mesenchymal tumor incidence, multiplicity, and size in Eker rats. [3] SB 525334 significantly reverses pulmonary arterial pressure and inhibits right ventricular hypertrophy in a rat model of PAH. This is revealed by a significant reduction in pulmonary arteriole muscularization induced by monocrotaline (used to induce PAH) after treatment with SB 525334 (3 or 30 mg/kg). [2] In a Bleomycin-induced pulmonary fibrosis mice model, SB 525334 (10 mg/kg or 30 mg/kg) attenuates the histopathological alterations in the lung, and significantly decreased mRNA expression of Type I and III procollagen and fibronectin. SB 525334 also attenuates Smad2/3 nuclear translocation, myofibroblast proliferation, deposition of Type I collagen, and decreases CTGF-expressing cells. [4]
Clinical Trials
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Kinase assay to determine the potency and selectivity of SB 525334 In order to determine the potency of SB 525334, purified GST-tagged kinase domain of ALK5 is incubated with purified GST-tagged full-length Smad3 in the presence of 33P-γATP and different concentrations of SB 525334. The readout is radioactively labeled Smad3. To determine the selectivity of SB 525334, purified GST-tagged kinase domain of ALK2 and ALK4 are incubated with GST-tagged full-length Smad1 and Smad3, respectively, in the presence of different concentrations of SB 525334. IC50 values are calculated.

Cell Assay: [1]

Cell lines Human renal proximal tubule epithelial (RPTE) cells
Concentrations 1 μM
Incubation Time 1 hour
Method RPTE cells are seeded on microscope slides. The following day, the cells are starved for 24 hours to dosing by removal of the serum and epidermal growth factor. Cells are treated with either 10 ng/mL TGF-β1, 1 μM SB 525334, or a combination of both. Slides are pretreated with SB 525334 or starve media for 3 hours prior to a 1-hour incubation at 37 °C with TGF-β1 or starve media. The cells are then fixed and permeabilized. The slides are blocked with BSA, incubated with a mouse anti-Smad2/3 primary antibody followed by an anti-mouse IgG fluorescein secondary antibody. The slides are then viewed in a confocal microscope and nuclear signal intensity is analyzed.

Animal Study: [3]

Animal Models Bleomycin-induced pulmonary fibrosis in female Eker rats
Formulation 200 mg/L in drinking water
Dosages Estimated dose of 10 mg/kg/day
Administration Oral (in drinking water)
1

References

Chemical Information

Download SB 525334 SDF
Molecular Weight (MW) 343.42
Formula

C21H21N5
CAS No. 356559-20-1
Synonyms N/A
Solubility (25°C)
  • DMSO 69 mg/mL
  • Water <1 mg/mL
  • Ethanol 69 mg/mL
Storage 2 years -20°CPowder
2 weeks4°Cin DMSO
6 months-80°Cin DMSO
Chemical Name 6-(2-tert-butyl-4-(6-methylpyridin-2-yl)-1H-imidazol-5-yl)quinoxaline
Molarity Calculator Dilution Calculator Molecular Weight Calculator

Research Area

Customer Reviews (1)


Click to enlarge 		Rating
Source SB 525334 purchased from Selleck
Method ALP assay/Quantitative RT-PCR
Cell Lines C3H10T1/2 cells
Concentrations 10 μM
Incubation Time
Results Cotreatment with SB-431542 or SB-525334 has not only inhibited ALP activities compared with vehicle treatment but also abrogated the TAZ-mediated enhancement of ALP activities.

Product Citations (2)

  • Osteoblast-Targeted Overexpression of TAZ Increases Bone Mass In Vivo. [Yang JY, et al. PLoS One 2013;8(2):e56585]

    PubMed: 23441207

  • Transforming growth factor beta receptor I inhibitor sensitizes drug-resistant pancreatic cancer cells to gemcitabine. [Kim YJ, et al. Anticancer Res 2012;32(3), 799-806]

    PubMed: 22399597

Tech Support & FAQs

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:3Monday–Friday 9:00 AM–5:00 PM (Central Time)

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

* Indicates a Required Field

Related TGF-beta/Smad Inhibitors

  • SB 431542

    SB 431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM.

  • SB-505124

    SB505124 is a selective inhibitor of ALK4 and ALK5 with IC50 of 129 nM and 47 nM, respectively.

  • LY2157299

    LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM.

  • LDN193189

    LDN193189 is a selective inhibitor of ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively.

  • LY2109761

    LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM, respectively.

  • GW788388

    GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM.

  • LY364947

    LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM.

  • Pirfenidone

    Pirfenidone inhibits TGF-β bioactivity by affecting TGF-β2 mRNA expression and processing of pro-TGF-β in CCL-64 cells.

  • Enzastaurin (LY317615)

    Enzastaurin (LY317615) is a potent PKC inhibitor for PKCβ, PKCα, PKCγ and PKCε with IC50 of 6 nM, 39 nM, 83 nM and 110 nM, respectively.

  • Staurosporine

    Staurosporine (AM-2282) is a potent PKC inhibitor with IC50 of 2.7 nM.

TGF-beta/Smad Pathway Products

> Download

Recently Viewed Items

Tags: buy SB 525334 | SB 525334 supplier | purchase SB 525334 | SB 525334 cost | SB 525334 manufacturer | order SB 525334 | SB 525334 distributor
Contact Us