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KYA1797K, Wnt/β-catenin Inhibitor

KYA1797K, Wnt/β-catenin Inhibitor

$129.00
A highly potent and selective Wnt/β-catenin inhibitor binding directly to the regulators of G-protein signaling domain of axin.
Catalog No. Unit Price Qty
M60317-2s 2 mg solid $129.00

Details

Product Information
Molecular Weight: 442.50
Formula: C17H11KN2O6S2
Purity: ≥98%
CAS#: n/a
Solubility: DMSO up to 100 mM
Chemical Name: potassium (Z)-3-(5-((5-(4-nitrophenyl)furan-2-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)propanoate
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 ~0.75 µM (TOPflash assay). It 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 GSK3β. KYA1797K can effectively suppress the growth of CRCs harboring APC and KRAS mutations, as shown by various in vitro studies and by in vivo studies using xenograft and transgenic mouse models of tumors induced by APC and KRAS mutations. Destabilization of both β-catenin and Ras via targeting axin is a potential therapeutic strategy for treatment of CRC and other type cancers activated Wnt/β-catenin and Ras pathways.

How to Use:


In vitro:
KYA1797K was suggested to be used at 25 µM final concentration in vitro.
In vivo: KYA1797K was used to dose mice at 20-25 mg/kg by intraperitoneal injection in xenograft model of D-MT cell line that harbors both APC and KRAS mutations, or in Apcmin/+/KrasG12D LA2 mouse model.

Reference:

  • 1. Cha PH, et al.Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation. (2016) Nat Chem Biol. 12(8):593-600. 

KYA1797K_spec.pdf 
KYA1797K_MSDS.pdf     


Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 442.50
Formula: C17H11KN2O6S2
Purity: ≥98%
CAS#: n/a
Solubility: DMSO up to 100 mM
Chemical Name: potassium (Z)-3-(5-((5-(4-nitrophenyl)furan-2-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)propanoate
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 ~0.75 µM (TOPflash assay). It 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 GSK3β. KYA1797K can effectively suppress the growth of CRCs harboring APC and KRAS mutations, as shown by various in vitro studies and by in vivo studies using xenograft and transgenic mouse models of tumors induced by APC and KRAS mutations. Destabilization of both β-catenin and Ras via targeting axin is a potential therapeutic strategy for treatment of CRC and other type cancers activated Wnt/β-catenin and Ras pathways.

How to Use:


In vitro:
KYA1797K was suggested to be used at 25 µM final concentration in vitro.
In vivo: KYA1797K was used to dose mice at 20-25 mg/kg by intraperitoneal injection in xenograft model of D-MT cell line that harbors both APC and KRAS mutations, or in Apcmin/+/KrasG12D LA2 mouse model.

Reference:

  • 1. Cha PH, et al.Small-molecule binding of the axin RGS domain promotes β-catenin and Ras degradation. (2016) Nat Chem Biol. 12(8):593-600. 

KYA1797K_spec.pdf 
KYA1797K_MSDS.pdf     


Products are for research use only. Not for human use.

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