| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
iCRT3 (iCRT-3) is an inhibitor of Wnt and β-catenin-responsive transcription in the Wnt/wingless signaling pathway with anticancer activity. It exhibits IC50 of 8.2 nM in the Wnt responsive STF16-luc reporter assays. iCRT3 can efficiently block Wnt/β-catenin-induced target genes and phenotypes in various mammalian and cancer cell lines. Importantly, these Wnt inhibitors are specifically cytotoxic to human colon tumor biopsy cultures as well as colon cancer cell lines that exhibit deregulated Wnt signaling. iCRT3 binds to β-catenin and interferes 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.
| ln Vitro |
iCRT3 inhibits transcription that is sensitive to both Wnt and β-catenin. Both TOP Flash activity and NTSR1 level are markedly lowered by iCRT3. iCRT3 can significantly counteract the anti-apoptotic effects of neurotensin (NTS) and Wnt3a[1]. Long-term iCRT3-maintained cells exhibit increased expression of classic pluripotency compared to the DMSO control, but concurrently decreased expression of differentiation markers and T-cell factor (TCF) target genes[2]. iCRT3 treatment reduces TNF-α levels by 14.7%, 18.5%, 44.9%, and 61.3% at dosages of 12.5, 25, 50, and 75 μM, respectively. IκB levels rise dose-dependently with iCRT3 therapy in contrast to the vehicle[3].
|
||
|---|---|---|---|
| ln Vivo |
Treatment with iCRT3 significantly reduces tumor growth rates. The tumor-suppressive function of iCRT3 is consistently correlated with a decrease in the proliferation marker Ki67 index[1]. Compared to the vehicle group, the IL-6 levels in the 10 mg/kg iCRT3 therapy group are 82.9% lower. In the sham, IL-1β levels are not detectable; however, in septic mice, they reach 371 pg/mL and decrease by 30.2% and 53.2%, respectively, when given 5 and 10 mg/kg iCRT3. The AST levels of these septic mice treated with iCRT3 at doses of 5 and 10 mg/kg are, respectively, 15.4% and 44.2% lower than those of the animals treated with vehicle. In comparison to the vehicle group, lung morphology improves with much less microscopic degradation following therapy with 10 mg/kg iCRT3. When comparing the lung tissues of the iCRT3-treated animals to the vehicle group, there are 92.7% fewer apoptotic cells[3].
|
||
| Animal Protocol |
|
||
| References |
[1]. Xiao H, et al. A Novel Positive Feedback Loop Between NTSR1 and Wnt/β-Catenin Contributes to Tumor Growth of Glioblastoma. Cell Physiol Biochem. 2017 Oct 24;43(5):2133-2142.
[2]. Chatterjee SS, et al. Inhibition of β-catenin-TCF1 interaction delays differentiation of mouse embryonic stem cells. J Cell Biol. 2015 Oct 12;211(1):39-51. [3]. Sharma A, et al. Mitigation of sepsis-induced inflammatory responses and organ injury through targeting Wnt/β-catenin signaling. doi: 10.1038/s41598-017-08711-6 |
| Molecular Formula |
C23H26N2O2S
|
|
|---|---|---|
| Molecular Weight |
394.53
|
|
| CAS # |
901751-47-1
|
|
| Related CAS # |
|
|
| SMILES |
O=C(NCCC1=CC=CC=C1)CSCC2=C(C)OC(C3=CC=C(CC)C=C3)=N2
|
|
| Chemical Name |
|
|
| Synonyms |
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Proc Natl Acad Sci U S A.2011 Apr 12;108(15):5954-63. |
|---|
Proc Natl Acad Sci U S A.2011 Apr 12;108(15):5954-63. |
Proc Natl Acad Sci U S A.2011 Apr 12;108(15):5954-63. |
Effect of iCRT3 administration on systemic cytokine levels after CLP.Sci Rep.2017 Aug 23;7(1):9235. |
|---|
Effect of iCRT3 treatment on the expression of cytokines in the lungs after CLP.Sci Rep.2017 Aug 23;7(1):9235. |
Effect of iCRT3 treatment on the neutrophil infiltration in the lungs after CLP.Sci Rep.2017 Aug 23;7(1):9235. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
