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677331-12-3

677331-12-3 structure
677331-12-3 structure
  • Name: iCRT-14
  • Chemical Name: (5Z)-5-[(2,5-dimethyl-1-pyridin-3-ylpyrrol-3-yl)methylidene]-3-phenyl-1,3-thiazolidine-2,4-dione
  • CAS Number: 677331-12-3
  • Molecular Formula: C21H17N3O2S
  • Molecular Weight: 375.44400
  • Catalog: Signaling Pathways Stem Cell/Wnt Wnt
  • Create Date: 2017-01-24 04:15:52
  • Modify Date: 2024-01-06 07:16:35
  • iCRT 14 is a novel potent inhibitor of β-catenin-responsive transcription (CRT), with IC50 of 40.3 nM against Wnt responsive STF16 luciferase.

Name (5Z)-5-[(2,5-dimethyl-1-pyridin-3-ylpyrrol-3-yl)methylidene]-3-phenyl-1,3-thiazolidine-2,4-dione
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.
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

[1]. Gonsalves FC, et al. An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway. Proc Natl Acad Sci USA. 2011 Apr 12;108(15):5954-63.

[2]. Bilir B, et al. Wnt signaling blockage inhibits cell proliferation and migration, and induces apoptosis in triple-negative breast cancer cells. J Transl Med. 2013 Nov 4;11:280.

Molecular Formula C21H17N3O2S
Molecular Weight 375.44400
Exact Mass 375.10400
PSA 80.50000
LogP 4.79500
Storage condition 2-8°C
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
RIDADR NONH for all modes of transport
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