6-CEPN
Based on 1 Customer Validation
6-CEPN is a RAS inhibitor. 6-CEPN can inhibit RAS activation by binding to Icmt binding sites. 6-CEPN has anticancer activity. 6-CEPN can block cancer cells in the G1 phase. 6-CEPN can induce autophagy and necrosis of Cancer cells (Icmt: isovalerylcysteine carboxymethyltransferase).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.17%
- CAS No.: 1054549-73-3
- Formule: C23H18O5
- Masse moléculaire:374.39
-
Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
IC50 & Target
P21[1].
In Vitro
6-CEPN (10-100 μM, 24 h) decreases cell activity in a dose-dependent manner in SW620, SW480, HCT116 and HT29 cells,and a can resist cell proliferation[1].
6-CEPN (10 μM, 24 h) can block the cell cycle in G1 phase in SW620 and HCT116 cells[1].
6-CEPN (10 μM, 24 h) induces cell necrosis in SW620 and HCT116 cells [1].
6-CEPN (2.5-10 μM, 24 h) induces autophagy and cell death of colon cancer cells by inhibiting RAS activation in SW620 and HCT116 cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:SW620, HCT116
-
Concentration:10 μM
-
Incubation Time:24 h
-
Result:Increased protein levels of p21 and decreased protein levels of p-Rb and cyclin D1 (P21, p-Rb, cyclin D1are cell cycle regulator associated with G1 phase).
-
Cell Line:SW620, HCT116
-
Concentration:2.5 μM, 5 μM, 10 μM
-
Incubation Time:24 h
-
Result:Resulted in the formation of red fluorescent acidic vesicular organelles and MDC-labelled particles (Key features of autophagy).
Increased the level of LC3 protein expression in cells and autophagy occurred.
-
Cell Line:SW620, HCT116
-
Concentration:2.5 μM, 5 μM, 10 μM
-
Incubation Time:24 h
-
Result:Significantly inhibited the phosphorylation of C-raf, ERK, AKT and mTOR, while had no significant effect on the levels of total C-raf, ERK, AKT and mTOR.
Inhibited RAS activation.
Strongly inhibited the activity of Icmt.
-
Cell Line:SW620, HCT116
-
Concentration:10 μM
-
Incubation Time:24 h
-
Result:Reduced cell viability by about 60%.
Chemical Information
-
CAS No. 1054549-73-3
-
Appearance Solid
-
Masse moléculaire 374.39
-
Formule C23H18O5
-
Color Light yellow to yellow
-
SMILES
O=C1CC(OC2=C1C(O)=C(C(O)=C2)/C=C/C3=CC=CC=C3)C4=CC=C(C=C4)O
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (267.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.68 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
-
Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
-
Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
-
Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
Pureté et documentation
-
Fiche technique (275 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Instruction de manipulation (2659 KB)
Références
[1]. Zhao Y, et al. 6-C-(E-phenylethenyl)naringenin induces cell growth inhibition and cytoprotective autophagy in colon cancer cells[J].European journal of cancer: official journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR), 2016, 68(Null). [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6710 mL | 13.3551 mL | 26.7101 mL | 66.7753 mL |
| 5 mM | 0.5342 mL | 2.6710 mL | 5.3420 mL | 13.3551 mL | |
| 10 mM | 0.2671 mL | 1.3355 mL | 2.6710 mL | 6.6775 mL | |
| 15 mM | 0.1781 mL | 0.8903 mL | 1.7807 mL | 4.4517 mL | |
| 20 mM | 0.1336 mL | 0.6678 mL | 1.3355 mL | 3.3388 mL | |
| 25 mM | 0.1068 mL | 0.5342 mL | 1.0684 mL | 2.6710 mL | |
| 30 mM | 0.0890 mL | 0.4452 mL | 0.8903 mL | 2.2258 mL | |
| 40 mM | 0.0668 mL | 0.3339 mL | 0.6678 mL | 1.6694 mL | |
| 50 mM | 0.0534 mL | 0.2671 mL | 0.5342 mL | 1.3355 mL | |
| 60 mM | 0.0445 mL | 0.2226 mL | 0.4452 mL | 1.1129 mL | |
| 80 mM | 0.0334 mL | 0.1669 mL | 0.3339 mL | 0.8347 mL | |
| 100 mM | 0.0267 mL | 0.1336 mL | 0.2671 mL | 0.6678 mL |
6-CEPN Related Classifications
HY-114569 Related Classifications
Powered by Bioz