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iCRT 14

Catalog No.GC16640

CRT inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

iCRT 14 Chemical Structure

Cas No.: 677331-12-3

Size Price Stock Qty
10mM (in 1mL DMSO)
$87.00
In stock
5mg
$79.00
In stock
10mg
$126.00
In stock
50mg
$532.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

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.

Background

iCRT 14 is a potent and specific inhibitor of β-catenin responsive transcription (CRT) with IC50 value of 40.3 nM [1].

iCRT 14 belongs to the thiazolidinedione class and is screened out by the dTF12-luciferase reporter assay. It inhibits the direct interaction between β-catenin and TCF4 and does not affect the interaction of β-catenin with other cognate protein partners. iCRT 14 also inhibits the mammalian Wnt responsive STF16 luciferase reporter in HEK293 cells with IC50 value of 40.3 nM. Besides that, iCRT 14 is specific against CRT over other conserved cell signaling pathways. It had no effect on the phosphorylation of Dvl induced by Wnt [1].

iCRT 14 can also interfere with TCF binding to DNA. Moreover, the inhibition of CRT resulted in the modulation of CRT-induced molecular and morphological changes including cell transformation phenotype and cell invasion. Furthermore, the treatment of HCT116 and HT29 cells with iCRT 14 exhibited cell cycle arrest in the G0/G1 phase. In the xenograft models of HCT116 and HT29, administration of iCRT 14 at dose of 50 mg/kg caused significant decrease in CycD1 and the subsequent suppression of tumor growth [1].

References:
[1] Gonsalves F C, Klein K, Carson B B, et al. An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway. Proceedings of the National Academy of Sciences, 2011, 108(15): 5954-5963.

Chemical Properties

Cas No. 677331-12-3 SDF
Formula C21H17N3O2S M.Wt 375.44
Solubility ≥ 18.75mg/mL in DMSO with ultrasonic and warming Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.6635 mL 13.3177 mL 26.6354 mL
5 mM 0.5327 mL 2.6635 mL 5.3271 mL
10 mM 0.2664 mL 1.3318 mL 2.6635 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 27 reference(s) in Google Scholar.)

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