SML0211
iCRT3
≥98% (HPLC), Wnt / b-catenin pathway inhibitor, powder
Synonym(s):
2-[[[2-(4-ethylphenyl)-5-methyl-4-oxazolyl]methyl]thio]-N-(2-phenylethyl)acetamide
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About This Item
Empirical Formula (Hill Notation):
C23H26N2O2S
CAS Number:
Molecular Weight:
394.53
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Product Name
iCRT3,
SMILES string
CCc1ccc(cc1)-c2nc(CSCC(=O)NCCc3ccccc3)c(C)o2
InChI key
QTDYVSIBWGVBKU-UHFFFAOYSA-N
InChI
1S/C23H26N2O2S/c1-3-18-9-11-20(12-10-18)23-25-21(17(2)27-23)15-28-16-22(26)24-14-13-19-7-5-4-6-8-19/h4-12H,3,13-16H2,1-2H3,(H,24,26)
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to tan
solubility
DMSO: ≥5 mg/mL
storage temp.
2-8°C
Quality Level
Related Categories
General description
iCRT3 is a small cell-permeable oxazole compound. It blocks cytokine secretion in lipopolysaccharide (LPS)-stimulated macrophages.
Application
iCRT3 has been used to inhibit the interactions between β-catenin and transcription factor (TCF).
iCRT3 has been used:
- for β- catenin inhibition in dual luciferase assay
- to inhibit β-catenin /TCF interactions and their transcriptional activity
- as wingless/tailess (wnt) antagonist, to determine Wnt/β-catenin signaling is essential for PROX1-mediated regulation of forkhead box protein C2 (FOXC2)(3)catenin inhibition in dual luciferase assay
- to inhibit β- catenin /TCF interactions and their transcriptional activity
- as wingless/tailess (wnt) antagonist, to determine Wnt/β-catenin signaling is essential for PROX1-mediated regulation of forkhead box protein C2 (FOXC2)
Biochem/physiol Actions
The key mediator of Wnt signaling is the transcriptional co-activator b-catenin. In the cytoplasm, b-catenin is tightly bound to a complex that includes Axin and GSK-3b. Stimulation causes b-catenin stabilization, translocation to the nucleus and association with TCF4 to initiate transcription of responsive genes, referred to as Catenin Responsive Transcription (CRT). Virtually all Wnt-associated cancers are the result of misregulated CRT. Three inhibitors of CRT (iCRT) were identified in a screen that employed RNAi based knockdown of Axin, which stimulates CRT without affecting upstream mechanisms such as GSK activity, transduction by disheveled / frizzled, etc. These compounds are potent inhibitors of CRT reporter genes, as well as endogenous gene targets. The compounds also disrupt b-catenin-TCF4 interaction in a dose dependent manner, and cause G0/G1 arrest in colon tumor lines.
Wnt / b-catenin pathway inhibitor
Storage Class
11 - Combustible Solids
wgk
WGK 3
Regulatory Information
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Mitigation of sepsis-induced inflammatory responses and organ injury through targeting Wntbeta-catenin signaling
Sharma A, et al.
Scientific reports, 7(1), 9235-9235 (2017)
UVB represses melanocyte cell migration and acts through beta-catenin
Bertrand JU, et al.
Experimental Dermatology, 26(10), 875-882 (2017)
Increasing beta-catenin/Wnt3A activity levels drive mechanical strain-induced cell cycle progression through mitosis
Benham-Pyle BW, et al.
eLife, 5, e19799-e19799 (2016)
Complementary Wnt Sources Regulate Lymphatic Vascular Development via PROX1-Dependent Wntbeta-Catenin Signaling
Cha B, et al.
Testing, 25(3), 571-584 (2018)
Archna Sharma et al.
Scientific reports, 7(1), 9235-9235 (2017-08-25)
The Wnt/β-catenin pathway has been involved in regulating inflammation in various infectious and inflammatory diseases. Sepsis is a life-threatening condition caused by dysregulated inflammatory response to infection with no effective therapy available. Recently elevated Wnt/β-catenin signaling has been detected in
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