1. TGF-beta/Smad
  2. TGF-β Receptor
  3. SB 525334

SB 525334 

Cat. No.: HY-12043 Purity: 99.96%
Handling Instructions

SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.

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

SB 525334 Chemical Structure

SB 525334 Chemical Structure

CAS No. : 356559-20-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 372 In-stock
Estimated Time of Arrival: December 31
100 mg USD 612 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    SB 525334 purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2017 Dec 18;1864(3):721-734.

    Microglial cells are incubated with or without TGF-β1 (5 ng/mL) and/or SB525334 (10 μM) for 24 h, followed by incubation with or without LPS for 24 h and subsequent NO determination.

    SB 525334 purchased from MCE. Usage Cited in: Cell Commun Signal. 2018 Dec 7;16(1):97.

    Immunofluorescence staining of LC3B and MHC in gastrocnemius in different groups (TGF-β1, TGF-β1+SB525334, SB525334, TGF-β1+CQ, TGF-β1+si-HMGB1) and HMGB1 staining of gastrocnemius.

    SB 525334 purchased from MCE. Usage Cited in: Cell Commun Signal. 2018 Dec 7;16(1):97.

    Western blot analysis of LC3B, p62, HMGB1 and MHC protein expression in gastrocnemius muscles with the treatment of groups (TGF-β1, TGF-β1+SB525334, SB525334, TGF-β1+CQ, TGF-β1+si-HMGB1).

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    • Customer Review

    Description

    SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.

    IC50 & Target

    IC50: 14.3 nM (ALK5)[1]

    In Vitro

    SB525334 (1 μM; for 15 minutes before stimulating with 0.625 ng/ml of TGF-β1, assesses after 6 days) inhibits TGF-β1-mediated proliferation of familial idiopathic pulmonary arterial hypertension (iPAH) pulmonary artery smooth muscle cells (PASMCs) at an IC50 of 295 nM [2].

    Cell Proliferation Assay[2]

    Cell Line: PASMC cells
    Concentration: 1 μM
    Incubation Time: Pre-incubated for 15 minutes (before stimulating with 0.625 ng/ml of TGF-β1), assessed after 6 days
    Result: Inhibited TGF-β1-mediated proliferation of familial iPAH PASMCs at an IC50 of 295 nM.
    In Vivo

    SB525334 (3-30 mg/kg; p.o.; daily from days 17 to 35) significantly reverses pulmonary arterial pressure in a rat model of pulmonary arterial hypertension (PAH)[2].

    Animal Model: Adult male Sprague-Dawley rats (MCT rat model of pulmonary hypertension)[2]
    Dosage: 3, 30 mg/kg
    Administration: Oral administration; daily from days 17 to 35
    Result: Reduced the proportion of fully muscularized vessels to 28% at 3 mg/kg and returned fully muscularized vessel distribution beyond that seen at day 17 and approaching the phenotype observed in saline-exposed controls at 30 mg/kg.
    Molecular Weight

    343.42

    Formula

    C₂₁H₂₁N₅

    CAS No.

    356559-20-1

    SMILES

    CC(C)(C1=NC(C2=CC=CC(C)=N2)=C(C3=CC=C4N=CC=NC4=C3)N1)C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 46 mg/mL (133.95 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.9119 mL 14.5594 mL 29.1189 mL
    5 mM 0.5824 mL 2.9119 mL 5.8238 mL
    10 mM 0.2912 mL 1.4559 mL 2.9119 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (6.06 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (6.06 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.96%

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    Product name:
    SB 525334
    Cat. No.:
    HY-12043
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