1956356-56-1
1956356-56-1 structure
- Name: KYA 1797K
- Chemical Name: KYA1797K
- CAS Number: 1956356-56-1
- Molecular Formula: C17H11KN2O6S2
- Molecular Weight: 442.507
- Catalog: Signaling Pathways Stem Cell/Wnt Wnt
- Create Date: 2018-02-22 10:33:07
- Modify Date: 2024-01-02 18:53:00
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KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC50 of 0.75 µM.
| Name | KYA1797K |
|---|---|
| Synonyms |
3-Thiazolidinepropanoic acid, 5-[[5-(4-nitrophenyl)-2-furanyl]methylene]-4-oxo-2-thioxo-, potassium salt, (5Z)- (1:1)
Potassium 3-[(5Z)-5-{[5-(4-nitrophenyl)-2-furyl]methylene}-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoate |
| Description | KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC50 of 0.75 µM. |
|---|---|
| Related Catalog | |
| 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]. |
| Cell Assay | 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]. |
| Animal Admin | 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]. |
| References |
| Molecular Formula | C17H11KN2O6S2 |
|---|---|
| Molecular Weight | 442.507 |
| Exact Mass | 441.969543 |
| Storage condition | -20℃ |