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iCRT3

Catalog No.GC19198 Copy One-Click Copy Product Info

iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription.

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iCRT3 Chemical Structure

Cas No.: 901751-47-1

Size Price Stock Qty
5mg
$54.00
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10mg
$88.00
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25mg
$161.00
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50mg
$295.00
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100mg
$503.00
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Sample solution is provided at 25 µL, 10mM.



Description of iCRT3

iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription.

iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription. iCRT3 significantly decreases TOP Flash activity and reduces the level of NTSR1. The anti-apoptotic effects of Neurotensin (NTS) and Wnt3a can be largely abrogated by iCRT3[1]. Cells maintained long term with iCRT3 show enhanced expression of classic pluripotency genes compare with the DMSO control, whereas expression of differentiation markers and T-cell factor (TCF) target genes is concomitantly reduced[2]. Treatment with iCRT3 at doses of 12.5, 25, 50, and 75 uM decreases TNF-α levels by 14.7%, 18.5%, 44.9% and 61.3%, respectively. With iCRT3 treatment, IκB levels are increased in a dose-dependent manner compare to the vehicle[3].

The tumor growth rates are markedly retarded by iCRT3 treatment. Consistently, the tumor-suppressive role of iCRT3 is accompanied with a reduction in Ki67 index, a proliferation marker[1]. The IL-6 levels in the 10 mg/kg iCRT3 treatment group are 82.9% lower than those in the vehicle group. IL-1β levels are undetectable in the sham but reach 371 pg/mL in septic mice and are down by 30.2% and 53.2%, respectively, with 5 and 10 mg/kg iCRT3. With iCRT3 treatment at doses of 5 and 10 mg/kg, AST levels in these septic mice are 15.4% and 44.2% lower, respectively, than those in the vehicle-treated mice. After treatment with 10 mg/kg iCRT3, lung morphology is improved with much reduced microscopic deterioration, compare to the vehicle group. The number of apoptotic cells in the lung tissues of the iCRT3-treated mice is significantly reduced by 92.7% in comparison with the vehicle group[3].

References:
[1]. Xiao H, et al. A Novel Positive Feedback Loop Between NTSR1 and Wnt/β-Catenin Contributes to Tumor Growth of Glioblastoma. Cell Physiol Biochem. 2017 Oct 24;43(5):2133-2142.
[2]. Chatterjee SS, et al. Inhibition of β-catenin-TCF1 interaction delays differentiation of mouse embryonic stem cells. J Cell Biol. 2015 Oct 12;211(1):39-51.
[3]. Sharma A, et al. Mitigation of sepsis-induced inflammatory responses and organ injury through targeting Wnt/β-catenin signaling. doi: 10.1038/s41598-017-08711-6.

Protocol of iCRT3

Cell experiment:

Cells are seeded into 96-well plates to a density of 5×103 cells per well and incubated in the culture medium with iCRT3 for an additional 48 h. Cell viability and cell apoptosis assays are carried out using a Cell Counting kit-8 and a Caspase-Glo 3/7 assay kit according to the manufacturer’s instructions, respectively[1].

Animal experiment:

NOD-SCID BALB/c mice are inoculated subcutaneously in the right back with 2×106 A172 cells. The growth of the primary tumors is recorded every 4 days. iCRT3 (5 mg/kg) is diluted in PBS i.p. triweekly when tumors grow to ~200 mm3. The control mice are treated with blank PBS containing 5% (v/v) DMSO. Tumor volume is evaluated with the following formula: volume=tumor length×width2/2. The mice are sacrificed 24 days after pharmaceutical treatment. The tumors are resected and embedded in paraffin, and the Ki67 staining is analyzed by immunohistochemistry[1].

References:

[1]. Xiao H, et al. A Novel Positive Feedback Loop Between NTSR1 and Wnt/β-Catenin Contributes to Tumor Growth of Glioblastoma. Cell Physiol Biochem. 2017 Oct 24;43(5):2133-2142.
[2]. Chatterjee SS, et al. Inhibition of β-catenin-TCF1 interaction delays differentiation of mouse embryonic stem cells. J Cell Biol. 2015 Oct 12;211(1):39-51.
[3]. Sharma A, et al. Mitigation of sepsis-induced inflammatory responses and organ injury through targeting Wnt/β-catenin signaling. doi: 10.1038/s41598-017-08711-6.

Chemical Properties of iCRT3

Cas No. 901751-47-1 SDF
Canonical SMILES O=C(NCCC1=CC=CC=C1)CSCC2=C(C)OC(C3=CC=C(CC)C=C3)=N2
Formula C23H26N2O2S M.Wt 394.53
Solubility DMSO : 150 mg/mL (380.20 mM) 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 of iCRT3

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1 mg 5 mg 10 mg
1 mM 2.5347 mL 12.6733 mL 25.3466 mL
5 mM 506.9 μL 2.5347 mL 5.0693 mL
10 mM 253.5 μL 1.2673 mL 2.5347 mL
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Review for iCRT3

Average Rating: 5 ★★★★★ (Based on Reviews and 37 reference(s) in Google Scholar.)

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