1. TGF-beta/Smad
  2. TGF-β Receptor

SB 525334 

Cat. No.: HY-12043 Purity: 99.45%
Handling Instructions

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

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
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 372 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 612 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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    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.
    • Biological Activity

    • Technical Information

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    • References

    Description

    SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6. IC50 value: 14.3 nM Target: ALK5 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].

    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.
    References
    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

    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

    Purity: 99.45%

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

    Cat. No.: HY-12043