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Chemical Structure| 901751-47-1 Chemical Structure| 901751-47-1

Structure of iCRT3
CAS No.: 901751-47-1

Chemical Structure| 901751-47-1

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iCRT3 can inhibit both Wnt and β-catenin-responsive transcription.

4.5 *For Research Use Only !

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Product Details of iCRT3

CAS No. :901751-47-1
Formula : C23H26N2O2S
M.W : 394.53
SMILES Code : O=C(NCCC1=CC=CC=C1)CSCC2=C(C)OC(C3=CC=C(CC)C=C3)=N2
MDL No. :MFCD14766288
InChI Key :QTDYVSIBWGVBKU-UHFFFAOYSA-N
Pubchem ID :6622273

Safety of iCRT3

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H302-H315-H318-H335
Precautionary Statements:P261-P280-P305+P351+P338
Class:8
UN#:3259
Packing Group:

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HCT116 cells 50 µM 1 day To validate the inhibitory effect of iCRT3 on Wnt target genes, iCRT3 significantly inhibited AXN2 and CYCD1 mRNA expression Proc Natl Acad Sci U S A. 2011 Apr 12;108(15):5954-63.
Mouse embryonic stem cells (mESCs) 10 µM 14 days ICRT3 treatment enhanced the expression of pluripotency markers and reduced the expression of differentiation markers in mESCs. J Cell Biol. 2015 Oct 12;211(1):39-51.
HCMEC/D3 20 µM 15 hours ICRT3 inhibited the binding of β-catenin to the transcription factor TCF-4 in hCMEC/D3 cells, resulting in significant reductions in the mRNA expression of claudin-3, claudin-5, Pgp, and BCRP, and decreased monolayer electrical impedance, indicating reduced tight junction integrity. Sci Rep. 2019 Dec 23;9(1):19718.
Drosophila Cl8 cells 9 ng/μL 16 hours To screen for inhibitors of the Wnt/β-catenin signaling pathway, iCRT3 significantly inhibited dTF12 reporter activity Proc Natl Acad Sci U S A. 2011 Apr 12;108(15):5954-63.
A549 cells 5 µM 24 hours ICRT3 significantly decreased the expression of LH3, Wnt1, β-catenin, and p-Smad3 proteins, and reduced collagen pyridine-crosslinking production. Arch Med Sci. 2019 Jan 16;16(2):436-445.
Mouse embryonic stem cells (mESCs) 10 µM 48 hours ICRT3 treatment reduced RA-induced differentiation and enhanced the expression of pluripotency markers. J Cell Biol. 2015 Oct 12;211(1):39-51.
C1.1 cells 10 µM 48 hours To investigate the effect of iCRT3 on TGF-β-induced cell migration and collagen expression. Results showed that iCRT3 combined with TGF-β significantly increased β-catenin/Foxo interaction, reduced β-catenin/TCF interaction, and decreased TGF-β-induced collagen expression. Am J Pathol. 2021 Jun;191(6):993-1009.
PLC/PRF/5 cells 200 µM 48 hours ICRT3 repressed the protein levels of TCF1, Survivin and PRC1 Mol Cells. 2018 Sep 30;41(9):830-841.
BT-549 25, 50, 75 µM 48 hours ICRT-3 effectively inhibits cell proliferation in BT-549 cells in a dose- and time-dependent manner. J Transl Med. 2013 Nov 4;11:280.
MDA-MB-231 25, 50, 75 µM 48 hours ICRT-3 effectively inhibits cell proliferation in MDA-MB-231 cells in a dose- and time-dependent manner. J Transl Med. 2013 Nov 4;11:280.
HCC-1143 25, 50, 75 µM 48 hours ICRT-3 effectively inhibits cell proliferation in HCC-1143 cells in a dose- and time-dependent manner. J Transl Med. 2013 Nov 4;11:280.
HCC-1937 25, 50, 75 µM 48 hours ICRT-3 effectively inhibits cell proliferation in HCC-1937 cells in a dose- and time-dependent manner. J Transl Med. 2013 Nov 4;11:280.
RAW264.7 macrophages 12.5, 25, 50, 75 µM 50 minutes pretreatment followed by 4 hours LPS stimulation ICRT3 significantly reduces LPS-induced Wnt/β-catenin activity and inhibits TNF-α production and IκB degradation in a dose-dependent manner. Sci Rep. 2017 Aug 23;7(1):9235.
HEK293 cells 25 µM To validate the inhibitory effect of iCRT3 on the Wnt signaling pathway, iCRT3 significantly inhibited STF16 reporter activity Proc Natl Acad Sci U S A. 2011 Apr 12;108(15):5954-63.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Unilateral renal ischemia reperfusion injury model Intraperitoneal injection 10 mg/kg Daily for 7 or 14 days To investigate the protective effect of iCRT3 on renal ischemia-reperfusion injury. Results showed that iCRT3 combined with TGF-β significantly increased β-catenin/Foxo interaction, reduced kidney fibrosis, and promoted tubular epithelial repair. Am J Pathol. 2021 Jun;191(6):993-1009.
C57BL/6 mice Cecal ligation and puncture (CLP)-induced sepsis model Intraperitoneal injection 5 and 10 mg/kg Single dose, administered 5 hours after CLP ICRT3 treatment significantly reduces plasma levels of proinflammatory cytokines and organ injury markers, and improves histological integrity of lung tissue, reducing lung collagen deposition and apoptosis. Sci Rep. 2017 Aug 23;7(1):9235.
Nude mice HCT116 and HT29 xenograft models Intraperitoneal injection 50 mg/kg Three times a week for 3 weeks To validate the anti-tumor effect of iCRT14 in vivo, iCRT14 significantly inhibited tumor growth Proc Natl Acad Sci U S A. 2011 Apr 12;108(15):5954-63.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.67mL

2.53mL

1.27mL

25.35mL

5.07mL

2.53mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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