iCRT3
SIGMA/SML0211
Synonym: 2-
CAS Number: 901751-47-1
Empirical Formula (Hill Notation): C23H26N2O2S
Molecular Weight: 394.53
MDL Number: MFCD14766288
Linear Formula: C23H26N2O2S
Product Type: Chemical
| assay | ≥98% (HPLC) |
| color | white to tan |
| form | powder |
| InChI | 1S/C23H26N2O2S/c1-3-18-9- |
| InChI key | QTDYVSIBWGVBKU-UHFFFAOYSA |
| Quality Level | 100  |
| SMILES string | CCc1ccc(cc1)-c2nc(CSCC(=O |
| solubility | DMSO: ≥5 mg/mL |
| storage condition | desiccated |
| storage temp. | 2-8°C |
| Application: | iCRT3 has been used to inhibit the interactions between β-catenin and transcription factor (TCF). |
| Application: | 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. |
| Biochem/physiol Actions: | Wnt / b-catenin pathway inhibitor |
| General description: | iCRT3 is a small cell-permeable oxazole compound. It blocks cytokine secretion in lipopolysaccharide (LPS)-stimulated macrophages. |
| Packaging: | 5, 25 mg in glass bottle |
| Hazard Codes | Xn |
| Risk Statements | 22-37/38-41 |
| Safety Statements | 26-39 |
| RIDADR | NONH for all modes of transport |
| WGK Germany | WGK 3 |
| Purity | ≥98% (HPLC) |
| Storage Temp. | 2-8°C |
| UNSPSC | 12352200 |