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KYA 1797K

Names

[ CAS No. ]:
1956356-56-1

[ Name ]:
KYA 1797K

[Synonym ]:
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

Biological Activity

[Description]:

KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC50 of 0.75 µM.

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> β-catenin
Signaling Pathways >> Stem Cell/Wnt >> Wnt
Research Areas >> Cancer

[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]

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


[Related Small Molecules]

XAV-939 | ICG-001 | Salinomycin | IWR-1 | Wnt-C59 | Berberine chloride hydrate | Pyrvinium pamoate | ETC-159 | BML 284 | IWP-2 | Heparan Sulfate | FH535 | SKL2001 | CCT251545 | iCRT-14

Chemical & Physical Properties

[ Molecular Formula ]:
C17H11KN2O6S2

[ Molecular Weight ]:
442.507

[ Exact Mass ]:
441.969543

[ Storage condition ]:
-20℃

Related Compounds