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

KYA1797K 

Cat. No.: HY-101090 Purity: ≥98.0%
Handling Instructions

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
25 mg USD 312 In-stock
Estimated Time of Arrival: December 31
50 mg USD 528 In-stock
Estimated Time of Arrival: December 31
100 mg USD 948 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 12 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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 b-catenin and Ras degradation through enhancement of the b-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].

    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 target [1].

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

    Molecular Weight

    442.51

    Formula

    C₁₇H₁₁KN₂O₆S₂

    CAS No.
    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
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 6 mg/mL (13.56 mM; Need ultrasonic)

    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
    10 mM 0.2260 mL 1.1299 mL 2.2598 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: 1 mg/mL (2.26 mM); Suspended solution; Need ultrasonic

    • 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

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

    KYA1797KWntβ-cateninBeta cateninInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
    HY-101090
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