1. Stem Cell/Wnt
  2. sFRP-1
  3. WAY 316606

WAY 316606 

製品番号: HY-10858 純度: 99.61%
取扱説明書

WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM.

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WAY 316606 構造式

WAY 316606 構造式

CAS 番号 : 915759-45-4

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 109 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 110 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 220 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 800 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1450 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    WAY 316606 purchased from MCE. Usage Cited in: Int J Dev Neurosci. 2018 May;66:24-32. 

    Whole-mount anti-5-HT (black) immunostaining of embryos treated with DMSO, WAY-316606, Sfrp1 protein, Sfrp1 plus WAY-316606, or Shh in utero electroporation together with WAY-316606 injection. Black arrows indicate misdirected axons.

    WAY 316606 purchased from MCE. Usage Cited in: Int J Dev Neurosci. 2018 May;66:24-32. 

    Quantification of the percentage of normal and misdirected 5-HT axons for the different groups.
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    製品説明

    WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM[1].

    IC50 & Target

    IC50: 0.5 μM (sFRP-1)[1]

    体外実験

    The EC50 of WAY-316606 for Wnt-Luciferase Activity from U2-OS Cells is 0.65 μM[1]. WAY-316606 binds to secreted frizzled-related protein (sFRP)-1 inhibitor with a KD of 0.08 μM and inhibits sFRP-1 with an EC50 of 0.65 μM. WAY-316606 also binds to sFRP-2, albeit over 10 times weaker with a KD of 1 μM. Using a fluorescence polarization binding assay that employs a fluorescent probe compound and purified human sFRP-1 protein in a competitive-binding format, the IC50 for WAY-316606 is 0.5 μM[2].

    体内実験

    WAY-316606 increases bone formation when tested in a neonatal murine calvarial assay. WAY-316606 increases total bone area up to 60% in a dose-dependent manner with an EC50 of about 1 nM. WAY-316606 has good aqueous solubility, moderate to low inhibition of cytochrome p450 isozymes (3A4, 2D6, 2C9) and good stability in rat and human liver microsomes (t1/2>60 min in each species). In female Sprague-Dawley rats, WAY-316606 exhibits high plasma clearance (77 mL/min/kg, greater than hepatic blood flow) following a single intravenous bolus dose (2 mg/kg), which results in a rapid decline of drug exposure in the plasma despite the route of administration[2].

    分子量

    448.48

    分子式

    C₁₈H₁₉F₃N₂O₄S₂

    CAS 番号

    915759-45-4

    SMILES

    O=S(C1=CC(S(=O)(C2=CC=CC=C2)=O)=CC=C1C(F)(F)F)(NC3CCNCC3)=O

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 100 mg/mL (222.98 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2298 mL 11.1488 mL 22.2975 mL
    5 mM 0.4460 mL 2.2298 mL 4.4595 mL
    10 mM 0.2230 mL 1.1149 mL 2.2298 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (5.57 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (5.57 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
    キナーゼ実験
    [2]

    WAY-316606 binding to purified sFRP is determined by spectroscopy methods. The sFRP-1 or -2 stock solutions are diluted to 1 μM in a buffered solution and the initial fluorescence is measured. Increasing concentrations of WAY-316606 (0 to 50 μM) are added to the protein in the cuvette and incubated for 5 min prior to assessing fluorescence intensity using a Fluoromax-2 fluorometer. In control experiments, the DMSO (vehicle control)-matched buffer solution is used. Fluorescence spectra are scanned in the ratio mode (S/R, signal/reference) to compensate for variations in lamp output as a function of wavelength. Fluorescence changes are fitted to a quadratic equation to obtain apparent dissociation constants[2].

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    細胞実験
    [1]

    U2OS bone cells are infected with recombinant adenovirus 5 (Ad5)−WNT3 at a multiplicity of infection (MOI) of 2, followed by infection with Ad5-sFRP-1 and Ad5-16xTCF-luciferase, each at an MOI of 10. Four hours after infection, the cells are frozen in sterile cryogenic vials at a cell density of 9×106 cells/mL and stored in a -150°C freezer. For the assay, a vial of frozen cells is thawed, and the cells are resuspended in plating medium to a final cell density of 1.5×105 cells/mL. The resuspended cells are then plated in 96-well tissue culture treated plates at a volume of 100 μL of cell suspension/well (i.e., 1.5×104 cells/well). The plates are incubated at 37°C inside a 5% CO2/ 95% humidified air incubator for 5 h or until the cells have attached and started to spread. Prior to the addition of WAY-316606, the medium is replaced with 50 μL/well of phenol red-free RPMI 1640. WAY-316606, or vehicle (typically DMSO), diluted in phenol red-free RPMI 1640 are then added to the wells in replicates of 4 wells/dilution and the plates are incubated at 37°C overnight. Dose−response experiments are performed with the compounds in 2-fold serial dilutions from 10000−4.9 nM. After the overnight incubation, the cells are washed twice with 150 uL/well of PBS w/o calcium or magnesium and lysed with 50 μL/well of 1× cell culture lysis reagent on a shaker at room temperature for 30 min. Aliquots of the cell lysates (30 μL) are transferred to 96-well luminometer plates, and the luciferase activity is measured in a MicroLumat PLUS luminometer using 100 μL/well of luciferase substrate.

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献
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    Keywords:

    WAY 316606WAY316606WAY-316606sFRP-1Secreted frizzled related protein 1SARP-2FrzAInhibitorinhibitorinhibit

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    製品名:
    WAY 316606
    製品番号:
    HY-10858
    数量:
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