2. GPCR/G Protein MAPK/ERK Pathway Cell Cycle/DNA Damage Autophagy
  3. Ras Cyclin G-associated Kinase (GAK) Autophagy
  4. 6-CEPN

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).

For research use only. We do not sell to patients.

6-CEPN Chemical Structure

6-CEPN Chemical Structure

CAS No. : 1054549-73-3

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5 mg USD 500 In-stock
10 mg USD 800 In-stock
25 mg USD 1600 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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)[1].

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.

6-CEPN Related Antibodies

Cell Cycle Analysis[1]

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 Autophagy Assay[1]

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.

Western Blot Analysis[1]

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 Viability Assay[1]

Cell Line: SW620, HCT116
Concentration: 10 μM
Incubation Time: 24 h
Result: Reduced cell viability by about 60%.
Molecular Weight

374.39

Formula

C23H18O5
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6710 mL 13.3551 mL 26.7101 mL
5 mM 0.5342 mL 2.6710 mL 5.3420 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (6.68 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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6-CEPN Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

6-CEPN1054549-73-3RasCyclin G-associated Kinase (GAK)AutophagyAuxilin 2Colon cancerNecrosisProliferationSW620SW480HCT116HT29Inhibitorinhibitorinhibit

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