KYA1797K - 10mM in DMSO , CAS No.1956356-56-1

CAS: 1956356-56-1 Cat. No.: K408253 Fórmula: C₁₇H₁₁KN₂O₆S₂ Peso molecular: 442.5

GRADE & PURITY 10mM in DMSO

Synonyms

3-​Thiazolidinepropanoi​c acid, 5-​[[5-​(4-​nitrophenyl)​-​2-​furanyl]​methylene]​-​4-​oxo-​2-​thioxo-​, potassium salt (1:1)​, (5Z)​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

Information

KYA1797K KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 of 0.75 µM (TOPflash assay).
In vitro

KYA1797K significantly decreases reporter activities for the Wnt/β-catenin and MAPK/ERK pathways but does not affect the reporter activities of other cancer-related pathways, such as the Notch and TGFβ pathways, thus, KYA1797K selectively regulates the Wnt/β-catenin and Ras/ERK pathways. KYA1797K enhances the β-catenin binding affinity of endogenous axin, GSK3β and β-TrCP. Interaction between APC and β-catenin is not enhanced by KYA1797K. It promotes the formation of the β-catenin destruction complex. KYA1797K degrades both β-catenin and Ras in these cells(CRC lines SW480, LoVo, DLD1 and HCT15) in a dose-dependent manner, cell proliferation is also suppressed by KYA1797K treatment. KYA1797K inhibits proliferation of CRC cells mainly via destabilization of β-catenin with additional Ras degradation. KYA1797K directly targeted axin and modulated conformation of the β-catenin destruction complex.

In vivo

KYA1797K administration by intraperitoneally injection(i.p.) (25 mg/kg) reduces both weight and volume of the tumor by 70% in mice carrying xenografted tumors from the D-MT cell line that harbors both APC and KRAS mutations. KYA1797K treatment significantly reduces levels of β-catenin and Ras proteins as well as Wnt/β-catenin and Ras signaling target. No change in the weight and no abnormalities in liver tissues of mice treated with KYA1797K. KYA1797K significantly reduces the subcellular localization of β-catenin in the nuclei and pan-Ras on the membrane of tumor cells. Thus, KYA1797K has anti-tumor effect.
Cell Data

cell lines：CHO cells expressing the h5-HT_1B or h5-HT_1D receptors

Concentrations：25 μM

Incubation Time：72 h

Powder Purity:≥99%

Specifications

Sinónimos

3-​Thiazolidinepropanoi​c acid, 5-​[[5-​(4-​nitrophenyl)​-​2-​furanyl]​methylene]​-​4-​oxo-​2-​thioxo-​, potassium salt (1:1)​, (5Z)​-

Especificações e pureza

10mM in DMSO

Mecanismos bioquímicos e fisiológicos

KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 of 0.75 µM (TOPflash assay).

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

INHIBITOR

Nomes e identificadores

• Peso molecular: 442.5
• Reaxy-Rn: 30137268
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=30137268&ln=

Perguntas frequentes

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1956356-56-1, the molecular formula is C??H??KN?O?S?, and the molecular weight is 442.5 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.