1. TGF-beta/Smad
  2. TGF-β Receptor
  3. SB-505124

SB-505124 

Cat. No.: HY-13521 Purity: 99.63%
Handling Instructions

SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.

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

SB-505124 Chemical Structure

SB-505124 Chemical Structure

CAS No. : 694433-59-5

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Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 158 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 504 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of SB-505124:

Top Publications Citing Use of Products

    SB-505124 purchased from MCE. Usage Cited in: Oncogene. 2019 Mar;38(12):2056-2075.

    Treatment with SB505124 for 3 days significantly increases apoptosis at 4 and 8 μM in WERI Rb1.

    SB-505124 purchased from MCE. Usage Cited in: Oncogene. 2019 Mar;38(12):2056-2075.

    Treatment with SB505124 for 3 days significantly increases apoptosis at 4 and 8 μM in WERI Rb1.

    SB-505124 purchased from MCE. Usage Cited in: Oncogene. 2019 Mar;38(12):2056-2075.

    The effects on growth and invasion are paralleled by a dose-dependent inhibition in SMAD2 phosphorylation upon treatment with SB505124 at 0.5, 1, 2, 3, 4, 8 μM for 4 days.

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    Description

    SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.

    IC50 & Target

    IC50: 129 nM (ALK4), 47 nM (ALK5)

    In Vitro

    SB-505124 demonstrates no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC50 value of 129±11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 μM. SB-505124 (1 μM) inhibits the TGF-β-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB-505124 (1 or 5 μM) potently inhibits TGF-β-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells[1]. SB-505124 (10 µM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro[2]. SB-505124 susspresses CTGF and α-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB-505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    SB-505124 (5 mg/kg; i.p.) alone has no effect in C57Bl6 mice with A549 xenografts, but administration of SB-505124 with a single dose of Carboplatin (60 mg/kg) results in durable responses without the need for maintenance therapy in five animals[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: C57Bl6 mice with A549 xenografts[4]
    Dosage: 5 mg/kg
    Administration: I.p.; daily
    Result: Had no effect alone, but administration with a single dose of carboplatin (60 mg/kg) resulted in durable responses without the need for maintenance therapy in five animals.
    Molecular Weight

    335.40

    Formula

    C₂₀H₂₁N₃O₂

    CAS No.
    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 : 113.33 mg/mL (337.90 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.9815 mL 14.9076 mL 29.8151 mL
    5 mM 0.5963 mL 2.9815 mL 5.9630 mL
    10 mM 0.2982 mL 1.4908 mL 2.9815 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: ≥ 2.5 mg/mL (7.45 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (7.45 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Product Name:
    SB-505124
    Cat. No.:
    HY-13521
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