| Identification | Back Directory | [Name]
2-[[[2-(4-ethylphenyl)-5-methyl-4-oxazolyl]methyl]thio]-N-(2-phenylethyl)acetamide | [CAS]
901751-47-1 | [Synonyms]
iCRT3
CS-2716
ICRT3;ICRT-3;ICRT 3
2-[[[2-(4-ethylphenyl)-5-methyl-4-oxazolyl]methyl]thio]-N-(2-phenylethyl)acetamide
Acetamide, 2-[[[2-(4-ethylphenyl)-5-methyl-4-oxazolyl]methyl]thio]-N-(2-phenylethyl)- | [Molecular Formula]
C23H26N2O2S | [MDL Number]
MFCD14766288 | [MOL File]
901751-47-1.mol | [Molecular Weight]
394.53 |
| Chemical Properties | Back Directory | [density ]
1.150±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥5mg/mL | [form ]
powder | [pka]
14.62±0.46(Predicted) | [color ]
white to tan |
| Hazard Information | Back Directory | [Uses]
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)
| [Uses]
iCRT3, is an inhibitor of both Wnt and β-catenin-responsive transcription (CRT). | [General Description]
iCRT3 is a small cell-permeable oxazole compound. It blocks cytokine secretion in lipopolysaccharide (LPS)-stimulated macrophages. | [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. |
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| Company Name: |
Sigma-Aldrich
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| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
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