Name | (5Z)-5-[(2,5-dimethyl-1-pyridin-3-ylpyrrol-3-yl)methylidene]-3-phenyl-1,3-thiazolidine-2,4-dione |
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Synonyms |
iCRT14
iCRT 14 |
Description | iCRT 14 is a novel potent inhibitor of β-catenin-responsive transcription (CRT), with IC50 of 40.3 nM against Wnt responsive STF16 luciferase. |
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Related Catalog | |
Target |
IC50: 40.3 nM (Wnt responsive STF16 luciferase)[1] |
In Vitro | iCRT14 can interfere with TCF binding to DNA in addition to its ability to influence TCF-β-cat interaction[1]. iCRT14 (10, 25, 50 μM) effectively inhibits cell proliferation in BT-549 cells in a dose- and time-dependent manner, but still less potent than iCRT3[2]. |
In Vivo | iCRT14 (50 mg/kg, i.p.) markedly decreases CycD1, proliferation of the tumors in HCT116 xenografts[1]. |
Cell Assay | Cells are seeded at 20,000 cells/well into 96-well plates. After overnight incubation, cells are treated with DMSO or each Wnt inhibitor (iCRT-3, 75 μM; iCRT-5, 200 μM; iCRT-14, 50 μM; IWP-4, 5 μM and XAV-939, 10 μM) for 48 hours. Cell viability is determined using the Cell Titer-Glo luminescent cell viability assay kit. Luminescence is measured using FLUOstar microplate reader. All treatments are performed in triplicate, and each experiment is repeated three times. |
References |
Molecular Formula | C21H17N3O2S |
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Molecular Weight | 375.44400 |
Exact Mass | 375.10400 |
PSA | 80.50000 |
LogP | 4.79500 |
Storage condition | 2-8°C |