| Identification | Back Directory | [Name]
4-[5-(3,4-DIMETHOXY-BENZYLIDENE)-4-OXO-2-THIOXO-THIAZOLIDIN-3-YL]-BUTYRIC ACID | [CAS]
18623-44-4 | [Synonyms]
iCRT5
iCRT-5
(iCRT5)
(Z)-4-(5-(3,4-dimethoxybenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)butanoic acid | [Molecular Formula]
C16H17NO5S2 | [MDL Number]
MFCD00703657 | [MOL File]
18623-44-4.mol | [Molecular Weight]
367.44 |
| Chemical Properties | Back Directory | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (up to 30 mg/ml) | [form ]
solid | [color ]
Yellow | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| Hazard Information | Back Directory | [Description]
iCRT5 (18623-44-4) is a selective CRT (β-catenin-responsive transcription) inhibitor.1? IC50=18 nM for Wnt responsive STF16 luciferase. Acts via interfering with the β-catenin, TCF4 interaction.1?Displays poor inhibition of cell proliferation in triple-negative breast cancer cells.2?Increases the surface expression of MHCII, CD80 and CD86 on unstimulated dendritic cells (DCs) with no detrimental effects on immune-phenotype of stimulated DCs.3?Modulators of Wnt signaling show great promise in animal models of several cancers.4?Cell permeable. | [Uses]
iCRT5 is a selective CRT (β-catenin-responsive transcription) inhibitor. | [References]
1) Gonsalves?et al.?(2011),?An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway; Proc. Natl. Acad. Sci. USA,?108?5954
2) Bilir?et al. (2013),?Wnt signaling blockage inhibits cell proliferation and migration, and induces apoptosis in triple-negative breast cancer cells; J. Transl. Med.,?11?280
3) Kafer?et al.?(2016),?Inhibitors of β-catenin affect the immune-phenotype and functions of dendritic cells in an inhibitor-specific manner; Immunopharmacol.,?32?118
4) Anastas?et al. (2013),?WNT signaling pathways as therapeutic targets in cancer; Nat. Rev. Cancer,?13?11 |
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