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]:

Signaling Pathways >> Stem Cell/Wnt >> Wnt

Research Areas >> Cancer

[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.

[Related Small Molecules]

ICG-001 | Salinomycin | IWR-1 | Wnt-C59 | Berberine chloride hydrate | Pyrvinium pamoate | ETC-159 | BML 284 | IWP-2 | Heparan Sulfate | KYA 1797K | FH535 | SKL2001 | CCT251545 | NCB-0846

[ Molecular Formula ]:
C₂₁H₁₇N₃O₂S

[ Molecular Weight ]:
375.44400

[ Exact Mass ]:
375.10400

[ PSA ]:
80.50000

[ LogP ]:
4.79500

[ Storage condition ]:
2-8°C

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ RIDADR ]:
NONH for all modes of transport

Sequential actions of β-catenin and Bmp pattern the oral nerve net in Nematostella vectensis.

Nat. Commun. 5 , 5536, (2014)

Animal evolution is closely linked to the emergence of the nervous system. At present it is unknown how the basic mechanisms of neural induction and formation of central nervous systems evolved. We ad...

A switch from canonical to noncanonical Wnt signaling mediates early differentiation of human neural stem cells.

Stem Cells 32(12) , 3196-208, (2014)

Wnt/β-catenin signaling is essential for neurogenesis but less is known about β-catenin-independent Wnt signals. We show here that Wnt/activator protein-1 (AP-1) signaling drives differentiation of hu...

Targeting Wnt pathway in mantle cell lymphoma-initiating cells.

J. Hematol. Oncol. 8 , 63, (2015)

Mantle cell lymphoma (MCL) is an aggressive and incurable form of non-Hodgkin's lymphoma. Despite initial intense chemotherapy, up to 50% of cases of MCL relapse often in a chemoresistant form. We hyp...

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