[CAS NO. 901751-47-1] iCRT3

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PRODUCTS SPECIFICATIONS [901751-47-1]

Catalog

SLK-S8647

Brand

Selleck

CAS

901751-47-1

DESCRIPTION [901751-47-1]

Overview

MDL	MFCD14766288
Molecular Weight	394.53
Molecular Formula	C23H26N2O2S
SMILES	O=C(NCCC1=CC=CC=C1)CSCC2=C(C)OC(C3=CC=C(CC)C=C3)=N2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.5347 mL	12.6733 mL	25.3466 mL
5 mM	0.5069 mL	2.5347 mL	5.0693 mL
10 mM	0.2535 mL	1.2673 mL	2.5347 mL
50 mM	0.0507 mL	0.2535 mL	0.5069 mL

Description

iCRT3 is an antagonist of signaling with an IC50 of 8.2 nM in the Wnt responsive STF16-luc reporter assays.

Targets

Wnt/β-catenin ^[1]
(in STF16 assay)

8.2 nM

In vitro

iCRT3 is a small molecule inhibitor of the Wnt pathway which binds to β-catenin interfering with its interaction with TCF. iCRT3 significantly reduces the LPS-induced Wnt/β-catenin activity and also inhibits TNF-α production and IκB degradation in a dose-dependent manner. iCRT3 does not influence the transcriptional activity of FOP-Flash luciferase reporter, which harbors mutations in the DNA binding sites for TCF (β-cat response element), showing specificity of the response. It inhibits cytokine production in LPS-stimulated macrophages.

In vivo

Intraperitoneal administration of iCRT3 to C57BL/6 mice, subjected to cecal ligation and puncture-induced sepsis, decreases the plasma levels of proinflammatory cytokines and organ injury markers in a dose-dependent manner. The histological integrity of the lungs is improved with iCRT3 treatment, along with reduced lung collagen deposition and apoptosis. In addition, iCRT3 treatment also decreases the expression of the cytokines, neutrophil chemoattractants, as well as the MPO activity in the lungs of septic mice.

References

[1] Gonsalves FC, et al. Proc Natl Acad Sci U S A. 2011, 108(15):5954-63.
[2] Sharma A, et al. Sci Rep. 2017, 7(1):9235.