SB525334

Catalog No.S1476

SB525334 Chemical Structure

Molecular Weight(MW): 343.42

SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM in a cell-free assay, 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.

Size Price Stock Quantity  
In DMSO USD 64 In stock
USD 70 In stock
USD 120 In stock
USD 470 In stock
USD 870 In stock
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Cited by 21 Publications

Purity & Quality Control

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Biological Activity

Description SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM in a cell-free assay, 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.
Targets
TGFβR1(ALK5) [1]
(Cell-free assay)
14.3 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
rhPOSTN NGjCSpNCeG:ydH;zbZMhSXO|YYm= MV:wMlXDqM7:TdMg MorzOFjDqGh? NE\lZ2l{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUhdnWvYnXyJI9nKGGyb4D0c5Rq[yClZXzsdy=> M3PsUVI1OTJ7MUi4
HUVECs MWLGeY5kfGmxbjDBd5NigQ>? M3f2V|ExKM7:TR?= MWeyOE81QC95MjDo NHWz[pFt\WGmczD0c{BiKGSrc4L1dJRqd25ib3[geIhmKEiXVlXDJI1wdm:uYYnldkBi\nSncjC3NkBpeg>? NXnFRopHOjN7Nki5PFE>
HUVECs M4W1[WZ2dmO2aX;uJGF{e2G7 MnTsNVAh|ryP M3vLWFczKGh? NV3vPFlM[myxY3vzJJNq\26jbHnu[y=> MXSyN|k3QDl6MR?=
HUVECs MVvGeY5kfGmxbjDBd5NigQ>? NWTLeVU{OTBizszN MoTZO|IhcA>? NHfFXlZz\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2Zic33h[FI> MXeyN|k3QDl6MR?=
MiaPaCa2 NFjweJlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYHSZlFFOC1zMDFOwG0> NEjtWWg4OiCq NVvlOGw4\W[oaXPp[Y51dHlicnXkeYNmeyC2aHWgeoli[mmuaYT5JJdqfGhiZ3XtZ4l1[WKrbnW= MV[yNlM6QTV7Nx?=
AsPC1 NYTNR2FpS2WubDDWbYFjcWyrdImgRZN{[Xl? MYWwMVExKM7:TR?= NHLsWHg4OiCq NEnEb3pm\m[rY3nlcpRtgSC{ZXT1Z4V{KHSqZTD2bYFjcWyrdImge4l1cCCpZX3jbZRi[mmwZR?= NYLD[WZuOjJ|OUm1PVc>
PASMCs  MlnSSpVv[3Srb36gRZN{[Xl? MYKxJO69VQ>? NUPZR3o{OTVibXnu MUjpcohq[mm2czDUS2Yu|rJzLX3l[IlifGWmIIDyc4xq\mW{YYTpc44hd2ZiZnHtbYxq[WxiaWDBTEBRSVOPQ4OgZZQh[W5iSVO1NOKhd2ZiMkm1JI5ud2xxTB?= NEjRfXMyQTFzNkO2NS=>
ELT-3  NYLNS3U2TnWwY4Tpc44hSXO|YYm= NYPjb2ZUOC53L{GuNE8zNjBizszN MXWxJIg> MlLaSG1UVw>? MorJbY5pcWKrdIOgWGdHNc7{IIPp[45idGmwZzDpckBt\WmxbYnvcYF{ NGqzZ2QyPzVyNUCxNi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Fibronectin / E-cadherin / Hif-1α ; 

PubMed: 29127306     


BEAS-2B cells were treated with NiCl2 (0.5 and 1 mM, respectively) or TGF-β (10 ng/ml) with or without SB525334 (10 μM) for 72 h and the protein levels were analyzed on Western blot. β-actin was used as the internal control. The relative ratios of Fibrone䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ

29127306
Immunofluorescence
E-cadherin / Vimentin; 

PubMed: 27471572     


Immunofluorescence analysis of EMT-related cell markers (200×). Red fluorescence indicates the epithelial marker E-cadherin, while green fluorescence indicates the mesenchymal marker vimentin. Cell nuclei are indicated in blue with DAPI. Our results show 䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙

27471572
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]

Protocol

Kinase Assay:[1]
+ Expand

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 Research:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • 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)
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 68 mg/mL (198.0 mM)
Ethanol 68 mg/mL (198.0 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.
20mg/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 343.42
Formula

C21H21N5

CAS No. 356559-20-1
Storage powder
in solvent
Synonyms N/A

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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.

Handling Instructions

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

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Frequently Asked Questions

  • Question 1:

    I want to know the feasibility of using the compound via oral gavage in rodents (dosing, frequency, formulation…)?

  • Answer:

    Our S1476 can be used for oral gavage in rodents, and the vehicle we suggest is: 30% Propylene glycol, 5% Tween 80, 65% D5W (dextrose(5%)in water) at 20mg/ml maximum. Based on the following reference they administrated it at an estimated dose of 10 mg/kg/day in rat for 2 months: http://clincancerres.aacrjournals.org/content/13/10/3087.long

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID