1. Stem Cell/Wnt
  2. Wnt β-catenin
  3. KYA1797K

KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC50 of 0.75 µM.

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

KYA1797K Chemical Structure

KYA1797K Chemical Structure

CAS No. : 1956356-56-1

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 92 In-stock
Solution
10 mM * 1 mL in DMSO USD 92 In-stock
Solid
5 mg USD 84 In-stock
10 mg USD 144 In-stock
25 mg USD 312 In-stock
50 mg USD 528 In-stock
100 mg USD 948 In-stock
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Customer Review

Based on 17 publication(s) in Google Scholar

Top Publications Citing Use of Products

    KYA1797K purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Sep 12;10(9):681.  [Abstract]

    Endometrial stromal cells are stimulated with 10 ng/mL TGFβ1 for 48 h. Then these cells are treated with 25 μM KYA1797K for 24 h and/or cocultured with 10 ng/mL VEGF165 for another 12 or 24 h. The protein levels of collagen 1, α-SMA and smad7 are examined.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC50 of 0.75 µM.

    IC50 & Target

    IC50: 0.75 (Wnt/β-catenin)[1]

    In Vitro

    KYA1797K binds directly to the regulators of G-protein signaling domain of axin, initiating β-catenin and Ras degradation through enhancement of the β-catenin destruction complex activating GSK3b. KYA1797K effectively suppresses the growth of CRCs harboring APC and KRAS mutations. KYA1797K enhances formation of the β-catenin destruction complex and induced GSK3β activation, leading to phosphorylation of both β-catenin and K-Ras at S33/S37/T41 and T144/T148. KYA1797K degrades both β-catenin and Ras SW480, LoVo, DLD1 and HCT15 cells in a dose-dependent manner. KYA1797K destabilizes β-catenin and Ras in DLD1 cells expressing WT β-catenin or WT K-Ras[1].

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

    In Vivo

    KYA1797K significantly suppresses tumor growth and progression both in mouse xenografts of CRC cells harboring APC and K-Ras mutations and in an Apcmin/+/KRASG12DLA2 mouse model. KYA1797K administration (25 mg/kg) reduces both weight and volume of the tumor by 70%. KYA1797K treatment significantly reduces levels of β-catenin and Ras proteins as well as Wnt/β-catenin and Ras signaling targets [1].

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

    Molecular Weight

    442.51

    Formula

    C17H11KN2O6S2

    CAS No.
    Appearance

    Solid

    Color

    Yellow to orange

    SMILES

    O=C(O[K])CCN(C/1=O)C(SC1=C/C2=CC=C(C3=CC=C([N+]([O-])=O)C=C3)O2)=S

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 6 mg/mL (13.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 1 mg/mL (2.26 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2598 mL 11.2992 mL 22.5984 mL
    5 mM 0.4520 mL 2.2598 mL 4.5197 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: 1 mg/mL (2.26 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: 1 mg/mL (2.26 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References
    Cell Assay
    [1]

    SW480, LoVo, DLD1 and HCT15 cells are treated with KYA1797K (0.2, 1, 5, 25 µM) for 24 h or 4 d. MTT assay is used to determine effects of KYA1797K on cell proliferation[1].

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

    Animal Administration
    [1]

    Mice: KYA1797K (20 mg/kg) is injected intraperitoneally (i.p.) into mice carrying xenografted tumors from the D-MT cell line that harbors both APC and KRAS mutations for 28 days. Tumor weight is measured at time of sacrifice and tumor volumes of mice are measured every 4 d[1].

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

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.2598 mL 11.2992 mL 22.5984 mL 56.4959 mL
    DMSO 5 mM 0.4520 mL 2.2598 mL 4.5197 mL 11.2992 mL
    10 mM 0.2260 mL 1.1299 mL 2.2598 mL 5.6496 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    KYA1797K Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    KYA1797K
    Cat. No.:
    HY-101090
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