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

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
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
25 mg USD 312 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 528 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 948 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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].

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].

References
Preparing Stock Solutions
Concentration Volume 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.
Cell Assay
[1]

KYA1797 is prepared in DMSO.

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]

KYA1797K is suspended in 90% PBS and 10% Tween 80.

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
Molecular Weight

442.51

Formula

C₁₇H₁₁KN₂O₆S₂

CAS No.

1956356-56-1

SMILES

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

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

Solvent & Solubility

DMSO: 6 mg/mL (Need ultrasonic)

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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