SB505124

Catalog No.S2186

SB505124 Chemical Structure

Molecular Weight(MW): 335.4

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.

Size Price Stock Quantity  
In DMSO USD 220 In stock
USD 170 In stock
USD 570 In stock
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Cited by 11 Publications

7 Customer Reviews

  • (D): Fluorescence micrographs of SOX2/FOXA2 double-staining of the conditions mentioned above. The TGF-b inhibitor SB-505124 (1 mM) was additionally used together with the complete medium. Nuclei were counterstained with DAPI. Original magnification 310 or 340. Abbreviations: DAPI, 40,6-diamidino-2-phenylindole; RA, retinoic acid.

    Stem Cells, 2016, 34:2635-2647.. SB505124 purchased from Selleck.

    Primary chondrocytes isolated from Cre-negative mice were pretreated with 1 μM SB-505124 for 30 min, followed by an additional 30 min incubation of 10 ng/ml TGF-β1, 10 μM H89/1 μM SB-505124, or a combination of both. Western blotting was performed to detect the pCREB protein expressions. Quantitative data were shown in the right panel (two-way ANOVA followed by Tukey’s test, n = 4 mice per group).

    Osteoarthritis Cartilage, 2017, 25(11):1868-1879. SB505124 purchased from Selleck.

  • FCS confirmed that SCH772984, SB505124 and Verteporfin administration apparently reduced the CD44 expression

    Oncotarget, 2016, 7(47):77495-77507. SB505124 purchased from Selleck.

    (C) The CTX-II release from the ECM of chondrocytes treated with/without 10 nM 1α,25(OH)2D3, TNF-α and TGF-β receptor inhibitor (SB505124). The effects of 1α,25(OH)2D3 on TNF-α stimulated chondrocytes were contracted by TGF-β receptor inhibitor. Values are the means ± 95% CI.

    Osteoarthritis Cartilage, 2016, 24(2):345-53. SB505124 purchased from Selleck.

  • Expression of NKILA assayed by qRT-PCR in A549 and H226 cells induced by TGF-β1 with or without TGF-β or NF-κB inhibition by SB505124 (SB) and JSH-23 (JSH) respectively.

    J Exp Clin Cancer Res, 2017, 36(1):54. SB505124 purchased from Selleck.

    TGF-b1 stimulates vimentin expression via Smad-signaling in U937 cells. Cells were stimulated with rhTGFb1 (0.2 ng/ml) after pretreatment with 0.2 nM SB505124 (an inhibitor of Smad2/3 phosphorylation) or 5 nM wortmannin (a PI3 K inhibitor). Total cell lysates was separated by SDS-PAGE and immunoblots were analyzed by Western blot. Cells without treatment belong to the control group. Histograms show the ratios of proteins to GAPDH. # p < 0.05 and ## P < 0.01 vs. the control group. ** P < 0.01 vs. the group treated with TGF-b1 alone

    Biomed Pharmacother, 2016, 83:1132-1140. SB505124 purchased from Selleck.

  • Total cell lysates was separated by SDS-PAGE and immunoblots were analyzed with specific antibodies after treatment with signaling inhibitors (0.2 nM SB505124, an inhibitor of Smad2/3 phosphorylation; 5 nM wortmannin, a PI3K inhibitor) for 30 min, cells were stimulated with rhTGF-β1 (0.2 ng/mL). Cells without treatment belong to the control group.

    Am J Chin Med, 2015, 43(1):183-98. SB505124 purchased from Selleck.

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
Sf9 insect cells NW\ubYJtTnWwY4Tpc44h[XO|YYm= Ml\TTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCJU2St[pV{\WRiQVzLOUBmgHC{ZYPz[YQhcW5iU3[5JIlve2WldDDj[YxteyC3c3nu[{Bk[XOnaX6gZZMhe3Wkc4TyZZRmKGK7IIDyc5BzcWW2YYL5JJJi\GmxaYPveI9xcWNicILveIVqdiCtaX7hd4Uh[XO|YYmsJGlEPTB;M{SuPUBvVQ>? NHXrNYMzPjR6M{G5PC=>
human HaCaT cells M4nFUWZ2dmO2aX;uJIF{e2G7 NHfhd5lKdmirYnn0bY9vKG:oIFHMT|UhcW5iaIXtZY4hUGGFYWSgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCWR1\i[ZRiOS2rbnT1Z4VlKGy3Y3nm[ZJie2ViYXP0bZZqfHliYX\0[ZIhOjRiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygTWM2OD12Mz64JI5O NIHrdGIzPDd6NkW4OS=>
mouse 4T1 cells MnnISpVv[3Srb36gZZN{[Xl? MnfyTY5pcWKrdHnvckBw\iCDTFu1JIlvKG2xdYPlJFRVOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHRITmKndHGxMYlv\HWlZXSgcJVkcW[ncnHz[UBi[3Srdnn0fUBi\nSncjCyOEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwQVc3NjZibl2= NIH3UmEzPDd6NkW4OS=>
mouse NMuMG cells MnqzSpVv[3Srb36gZZN{[Xl? MoHRNE4yNTBwNTFOwG0> M3rWe|EhcA>? NEDZdnJKdmirYnn0bY9vKG:oIFHMT|Uh[WO2aY\peJkhcW5ibX;1d4UhVk23TVegZ4VtdHNiYYPz[ZN{\WRiYYOgWGdH[mW2YT3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDTcYFlOiCjdDCwMlEhfG9iMD61JJVOKGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MmDDNlMxPDd{Mk[=

... 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).
  • Formulation: Tablets containing 5 mg of SB505124 and 65 mg lactose (6 mm in diameter, 1.0 mm in thickness) are prepared using a compression technique.
  • 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):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing. 		10 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

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Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID